INTRODUCTION:Flavone derivatives are naturally occurring compounds with diverse biological activities, including anticancer effects. However, the anticancer potential of sulfonamide-substituted flavones remains largely unexplored. MATERIALS AND METHODS:Compounds 7a-7l were synthesized via Claisen-Schmidt condensation of N-(3-acetyl-4-hydroxyphenyl)acetamide with various aromatic aldehydes. Structural characterization was performed using 1H, 13C, and 19F NMR spectroscopy, LC-MS, and elemental analysis. Molecular docking was conducted using AutoDock Vina, with input files prepared via AutoDockTools (ADT). The pharmacokinetic properties of compound 7f were predicted in silico using the PreADMET web tool. RESULTS:Among the synthesized compounds, 7f exhibited the highest anticancer activity against the NCI-60 panel, with GI50 values ranging from 0.58 to 14.6 μM and total growth inhibition (TGI) values from 9.17 μM to >100 μM. The strongest activity was observed against leukemia (K-562, GI50 = 0.58 μM), melanoma (MDA-MB-435, GI50 = 1.03 μM), renal (TK-10, GI50 = 1.08 μM; A498, GI50 = 1.88 μM), lung (HOP-92, GI50 = 1.34 μM), and CNS (SNB-75, GI50 = 1.63 μM) cancer cell lines. Low cytotoxicity was observed for most subpanels (LC50 > 100 μM). Molecular docking analysis suggested poly( ADP-ribose) polymerases (PARP1, TNKS1, and TNKS2) as potential molecular targets, with TNKS1 exhibiting the most favorable binding affinity (ΔG = -11.1 kcal/mol). in silico ADME predictions indicated a favorable pharmacokinetic profile. DISCUSSION:A series of sulfonamide-flavone hybrids was designed, synthesized, and evaluated using a combination of in vitro and in silico approaches. The results support the flavone-sulfonamide scaffold as a viable platform for further anticancer drug development. CONCLUSION:In summary, twelve novel flavone-sulfonamide hybrids were successfully synthesized and characterized. Biological evaluation identified compound 7f as the most active derivative against the NCI-60 panel, exhibiting broad-spectrum anticancer activity with low cytotoxicity. Molecular docking and ADME analyses further supported its potential, identifying compound 7f as a promising lead compound for further optimization. Incorporation of a sulfonamide group at the 6-position of the flavone scaffold resulted in an eightfold increase in anticancer activity (GI), from 7% for the flavone to 55% for lead compound 7f.

Introduction: Seven new 4-[2-(dichloromethyl)pyrazolo[1,5-a][1,3,5]triazine derivatives were investigated for anticancer activity, possible molecular mechanisms of anticancer action, and ADMET properties. Methods: The 4-benzenesulfonamide derivatives of pyrazolo[1,5-a][1,3,5]triazine were synthesized using the condensation of N-(2,2-dichloro-1-cyanovinyl)-amides IV with 1H-pyrazol-5-amine. Compound antitumor activities were evaluated using the NCI-60 human cancer cell line. AutoDockTools and AutoDock Vina software were used for molecular modeling. Using the ADMETlab 3.0 and pkCSM web sources, the ADMET properties of compounds 4, 5, and 7 were calculated. Results: Seven new pyrazolo[1,5-a][1,3,5]triazine derivatives were synthesized. The compounds 4, 5, and 7 exhibit high activity >1 μM against leukemia, colon, and renal cancer. Compound 4 exhibited the most potent activity, with IC50 values of 0.32 μM against leukemia, 0.49-0.89 μM against colon cancer, and 0.92 μM against renal cancer. Molecular modeling has demonstrated a potential antitumor mechanism involving CDK. The predicted ADMET profile of compounds 4, 5, and 7 is favorable. Discussion: The seven novel pyrazolo[1,5-a][1,3,5]triazines, as purine bioisosteres, were developed, synthesized, and investigated by in vitro and in silico methods. Conclusion: Seven novel pyrazolo[1,5-a][1,3,5]triazine derivatives exhibited anticancer activity against the NCI-60 cancer cell lines. The compounds 4, 5, and 7 demonstrated strong anticancer activity, with growth inhibition (GI) values exceeding 50% across all nine cancer types tested. The most active compound, 4, is against leukemia, colon cancer, renal cancer, and lung cancer. All compounds exhibit low toxicity, with LC50 values of 100 μM or greater. The molecular docking of compounds 4, 5, and 7 revealed the potential to inhibit cancer-associated cyclin-dependent kinases. The predicted ADMET profiles of their compounds are favorable, providing a basis for further improvement of their anticancer activity.

Bacterial infections contribute to many human diseases and cancer development, and their increasing incidence, together with rising antimicrobial resistance, underscores the urgent need for new potent biologically active compounds. Quantitative structure-activity relationship (QSAR) modeling was conducted to evaluate a series of oxazole derivatives as antibacterials. Eighteen new 5-amino-4-cyano-1,3-oxazoles with promising predictive properties were synthesized and reliably characterized. Fourteen compounds were found to inhibit bacterial growth (MICs varied from 8 to 512 µg/mL). Eight derivatives exhibited the highest activity against colistin-resistant Escherichia coli and Staphylococcus aureus isolates with MICs of 8-64 µg/mL. Moreover, six compounds exhibited activities greater or similar to that of reference oxacillin and cefepime against clinical isolates. Analysis of the studied 5-amino-4-cyano-1,3-oxazoles as target-directed glutathione S-transferase (GST) inhibitors showed that derivatives 7, 11, and 12 inhibited GSTA1-1 with an IC50 range of 3.2-7.5 µM. Molecular docking results indicate that these compounds can occupy the enzyme's active site. The cytotoxicity results in L20B and RD cell lines showed that compounds 11 and 12 demonstrated significant cytostatic effects, with CD50 values ranging from 0.02 to 2 µg/mL. Additionally, these two compounds showed moderate acute toxicity toward D. magna, with LC50 values of 7.27 ± 1.22 and 5.10 ± 1.07 mg/L (D.R. Passino classification).

An efficient approach to the multigram synthesis of 2-((hetera)cyclo)alkylchromanols and their spirocyclic analogs based on enzymatic resolution is described. It is shown that enzymatic acylation could be used for the preparation of enantioenriched title compounds with primary alkyl substituents at the C-2 position. Meanwhile, enzymatic hydrolysis of the corresponding acetates was optimal for the synthesis of the target alcohols when significant steric hindrance is present, e.g., due to the -branching. The latter factor was demonstrated to be crucial for the enzymatic reaction rate in both cases. The synthetic utility of the obtained chiral alcohols was demonstrated through Mitsunobu configuration inversion, as well as by the preparation of the corresponding primary amines – valuable sp3-enriched building blocks for medicinal chemistry.

Background: Indole is considered the most promising scaffold for anticancer drug design due to its high bioavailability, unique chemical properties, and broad spectrum of pharmacological action. Objective: Twelve novel thiazole-containing the 5-fluoro-1,3-dihydro-2H-indol-2-one derivatives as sunitinib analogs were designed and synthesized, and their anticancer activity was evaluated against the NCI-60 cancer cell lines. Method: The thiazole-contained 5-fluoro-1,3-dihydro-2H-indol-2-one derivatives were synthesized using Knoevenagel condensation of 1,3-thiazole-5-carboxylic acid 1. Their anticancer activities were evaluated by NCI-60 one-dose screen assay. The molecular docking studies were performed using AutoDock tools and the AutoDock Vina programs. The ADMETlab 2.0 web server predicted the physicochemical properties of compounds. Results: Among the synthesized new 5-fluoro-2-oxindole derivatives, compound 3g demonstrated high antitumor activity (GI>70%) against eight types of cancer: leukemia, breast cancer, ovarian cancer, lung cancer, melanoma, CNS cancer, renal cancer, and colon cancer. The most activity was observed against breast cancer (T-47D, GI=96.17%), lung cancer (HOP-92, GI=95.95%), ovarian cancer (NCI/ADR-RES, GI=95.13%), and CNS cancer (SNB-75, GI=89.91%). The molecular docking results of compound 3g demonstrated the possibility of inhibiting VEGF2 receptors as his potential anticancer mechanism. The physicochemical properties predicted for compounds 3f and 3g showed positive results. Conclusion: Compound 3g demonstrated high in vitro NCI-60 anticancer activity against nine cancer types and showed cell growth inhibition against leukemia, CNS, and breast cancer at 6 - 31% higher than Sunitinib, and may represent the basis for further modification of the thiazole-containing analogs of the anticancer drug Sunitinib.

A twenty six 7-amino[1,2,5]oxadiazolo[3,4-b]pyridine-6-carboxylate (7-aminofurazano[3,4-b]pyridine-6carboxylate) derivatives have been synthesized and characterized by IR, 1H NMR, 13C NMR spectroscopy, elemental analysis and LC-MS. The potential vasodilator activity of the synthesized compounds was assessed for their ability to induce relaxation of phenylephrine-precontracted isolated rat aortic segments. Eight derivatives showed high vasorelaxant activity, ranging from 73.7 to 87.3 %. Six samples contained an ethyl carboxylate moiety at the 6th position and alkyl or cycloalkyl substituents at the 5th position. Moreover, in the series of compounds with n-alkyl and cycloalkyl substituents, the derivative activity decreased linearly as the number of carbon atoms diminished. ADMET analysis showed that the highly active derivatives met the requirements for drug candidates regarding bioavailability, physicochemical and pharmacokinetic properties. These compounds are also approved by all the filters used, such as druglikeness and leadlikeness. The only problematic property of these highly active vasorelaxants is their in silico predicted very high carcinogenicity, which may be incompatible with their long-term use. Seven derivatives exhibited high virtual similarity to acetylcholinesterase inhibitors, with scores in the range of 0.857 to 0.932. This suggests that they may increase acetylcholine levels, thereby reducing vascular tone. However, this requires experimental confirmation. It should be noted that some 7-aminofurazano[3,4-b]pyridine-6-carboxylate analogs showed a high similarity to inhibitors of adenosine receptors, the non-receptor protein tyrosine kinases JAK2 and JAK3, glycogen synthase kinase-3 beta, prostaglandin E synthase and arachidonate 5-lipoxygenase, providing a basis for direct virtual assessment of their interaction with these targets. The results obtained highlight the considerable potential for further development of this class of compounds as vasoactive agents.

An efficient approach to the multigram synthesis of 3-azabicyclo[3.1.1]heptanes is described. The method relied on the intramolecular imide formation in the properly 1,3-functionalized cyclobutane derivative. In turn, the latter compound was obtained via the diastereoselective Strecker reaction of readily accessible 3-oxocyclobutanecarboxylate. The resulting synthetic intermediate – 1-amino-3-azabicyclo[3.1.1]heptane-2,4-dione – was used to synthe¬size several monoprotected bicyclic diamines valuable as building blocks for medicinal chemistry, as well as a series of bridged analogs of Thalidomide, a known anticancer drug and a component of proteolysis-targeting chimeras (PROTACs).

In the present study, eight novel substituted 4‐cyano‐ N ‐(4‐cyano‐1,3‐oxazol‐5‐yl)‐ N ‐alkyl‐1,3‐oxazole‐5‐sulfonylamides have been synthesized. Compounds are characterized by IR, 1 H, 13 C NMR spectroscopy, elemental analysis, and chromato‐mass‐spectrometry. The anticancer activities of six compounds are evaluated against the NCI‐60 human tumor cell line panel. The tested compounds exhibit the strongest antiproliferative (TGI) and cytotoxic (LC 50 ) activities within the leukemia, non‐small‐cell lung cancer, melanoma, and colon cancer subpanels. Overall, the mean activity parameters (GI 50 , TGI, and LC 50 ) calculated for three compounds do not differ significantly and are within the range of 1–100 µM, and for some lines, it reaches the value 10 −8 mol L −1 . Structure–activity relationship analysis reveals markedly higher activity for bisoxazole derivatives bearing 4‐MeC 6 H 4 or 4‐FC 6 H 4 at the second position of the oxazole rings (compounds 2 , 3 , and 7 ), whereas derivatives with diphenyl, di‐tolyl substituents (compounds 1 and 6 ), or 4‐ClC 6 H 4 (compound 8 ) exhibit substantially lower anticancer activity. In addition, the potential molecular mechanisms of anticancer action of these compounds are investigated using molecular docking methods. Derivatives show the highest affinity for tubulin and cyclin‐dependent kinases. Docking of 4‐cyano‐ N ‐[4‐cyano‐2‐(4‐fluorophenyl)‐1,3‐oxazol‐5‐yl]‐ N ‐methyl‐2‐(4‐methylphenyl)‐1,3‐oxazole‐5‐sulfonamide into the colchicine‐binding site of αβ‐tubulin reveals a binding affinity of −10.9 kcal mol −1 , with the ligand located at the subunit interface.

Phytophthora infestans control is a long-standing problem that has caused ongoing difficulties and brought limited success for over a century. Traditional methods, such as fungicides, have drawbacks including high cost, restrictions on organic farming, potential risks to the environment and human health, and the development of resistant strains. In this study, we employed cutting-edge computer-based techniques, including Quantitative Structure-Activity Relationship (QSAR) modeling and molecular docking simulations, to uncover new fungicidal compounds and gain insights into their specific mechanisms of action against P. infestans. QSAR modeling on the number of compounds tested as P. infestans inhibitors was performed using an interactive OCHEM web platform. The predictive ability of the developed classification models had a balanced accuracy (BA) of 77-85 % for the training set and BA 1/4 89-93 % for the validation external test set. During the in vitro testing against P. infestans, thirteen synthesized 2-oxoimidazolidine-4-sulfonamides demonstrated inhibition rates, ranging from 23.6 % to 87.4 %. The fungicidal potential of six of these fungicides ranged from 79.3 % to 87.4 %, which is comparable to the activity of known fungicides. Acute toxicity results using the well-known aquatic marker Daphnia magna showed that the most active sulfonamides 3d, 3f, 3h, 3j, 3k, and 3l, with LC50 values ranging from 13.7 to 52.9 mg/L, are low-toxicity compounds. The molecular docking results demonstrated a potential mechanism of the antifungal action of the studied 2-oxoimidazolidin-4-sulfonamide derivatives via the inhibition of fungal CYP51, a sterol biosynthesis enzyme.

This report presents a comprehensive overview of the meticulous construction of a series of classification structure–activity relationship (SAR) models. These models are specifically designed to accurately predict the antibacterial activity of untested compounds against Acinetobacter baumannii . The binary models are based on 1687 chemicals and demonstrate a broad applicability domain for the structures for which they were designed. External validation with a test set confirms the models' capability to accurately predict the activity of newly designed compounds within the applicable range, achieving an accuracy of 78%–84%. The models were used to perform a virtual screening of a chemical library for compounds expected to be active against Acinetobacter baumannii . Six of the most promising compounds were synthesized and evaluated in vitro to assess their antibacterial activity. All tested molecules revealed high anti‐ A. baumannii activity. Our findings indicate that 3‐oxazol‐4‐yl phosphonium salts demonstrate significant cytotoxicity. Notably, these compounds have been identified as potent anticancer agents, exhibiting IC 50 values ranging from 0.005 to 11.49 µM against the HEp‐2 cell line.

A number off[4-(diethoxyphosphoryl)-2-R-1,3-oxazol-5-yl]aminogalkyl methanesulfonates were synthesized and the peculiarities of their reaction with triethylamine were studied. The influence of the structure of the 5-alkanolamine substituent on the efficiency of their transformation into 7-R-1-ethoxy-5-methyl-1,3,4,5-tetrahydro-1?(5)-[1,3]oxazolo[4,5-c][1,5,2]oxazaphosphepine-1-ones was clarified. The structure of the [1,3]oxazolo[4,5-c][1,5,2]oxazaphosphepine derivatives has been reli-ably proven by elemental analysis, IR, H-1, C-13, and P-31 NMR spectroscopy (including 1D and 2D experiments), mass spectrometry and single crystal X-ray diffraction. The oxazole cycle in [1,3]oxa-zolo[4,5-c][1,5,2]oxazaphosphepines is easily cleaved by water in an acidic environment, which leads to the formation of derivatives of the new heterocyclic system - N-(2-ethoxy-5-methyl-2-oxido-4-oxo-1,5,2-oxazaphosphepan-3-yl)arylamides.

The regulatory effect of new synthetic thienopyrimidine derivatives on the growth and photosynthesis of wheat (Triticum aestivum L.) variety Svitlana in the vegetative phase was studied. The regulatory effect of new synthetic thienopyrimidine derivatives was compared with the regulatory effect of auxin IAA (1H-indol-3-yl)acetic acid) or synthetic plant growth regulators Methyur (sodium salt of 6-methyl-2-mercapto-4-hydroxypyrimidine) and Kamethur (potassium salt of 6-methyl-2-mercapto-4-hydroxypyrimidine). After 2 weeks, morphometric parameters (such as average length of shoots and roots (mm), average biomass of 10 plants (g)) and biochemical parameters (such as content of photosynthetic pigments (µg/ml)) of wheat plants grown from seeds treated with synthetic thienopyrimidine derivatives, or auxin IAA, or synthetic plant growth regulators Methyur and Kamethur at a concentration of 10-6M, were measured and compared with similar parameters of control wheat plants grown from seeds treated with distilled water. The regulatory effect of new synthetic thienopyrimidine derivatives on the morphometric and biochemical parameters of wheat plants was similar or higher compared to the regulatory effect of auxin IAA, or synthetic plant growth regulators Methyur and Kamethur. The relationship between the chemical structure of new synthetic thienopyrimidine derivatives and their regulatory effect on the growth and photosynthesis of wheat plants was revealed. The most biologically active thienopyrimidine derivatives are proposed to be used as new synthetic physiological analogues of auxins and cytokinins to improve growth and increase photosynthesis of wheat (Triticum aestivum L.) variety Svitlana in the vegetative phase.

The work is devoted to the screening of new effective wheat plant growth regulators based on synthetic compounds, thioxopyrimidine derivatives. The wheat (Triticum aestivum L.) variety Oksamit Mironivskyi was used as the object of the study. Morphometric parameters (average length of shoots and roots (mm), and average biomass of 10 plants (g)) of 4-week-old wheat plants were measured. Treatment of wheat plants with thioxopyrimidine derivatives at a concentration of 10-6 M contributed to the growth and development of shoots and roots compared to control wheat plants treated with distilled water. The regulatory effect of thioxopyrimidine derivatives on the vegetative growth of wheat plants was similar to the regulatory effect of auxin IAA (1H-indol-3-yl)acetic acid) or synthetic compounds, derivatives of sodium and potassium salts of 6-methyl-2-mercapto-4-hydroxypyrimidine (Methyur, Kamethur) and N-oxide-2,6-dimethylpyridine (Ivin) used in the same concentration of 10-6 M. The correlation between the growth regulatory effect and the chemical structure of synthetic compounds, thioxopyrimidine derivatives was established. The selected most active synthetic compounds, thioxopyrimidine derivatives, are proposed to be used to improve the vegetative growth of wheat (T. aestivum L.) variety Oksamit Mironivskyi.

On the base of 3-formylpicolinic acid by two successive heterocyclizations (the formation of a pyrone fragment by the cyclization of chloroacetone with the carboxyl and formyl groups; and the construction of the thiazole cycle through the bromination of the acetyl fragment and following interaction with thioamides), 6-(2-(phenyl/thiophen-2-yl)thiazole-4-yl)-8H-pyrano[3,4-b]pyridin-8-ones were obtained; and then the pyrone fragment was converted to pyridone by the action of ammonia under high pressure. When such 6-(2-R-thiazol-4-yl)-1,7-naphthyridin-8(7H)-ones reacted with triflic anhydride, O-sulfonylation of the pyridone fragment occurred, after that triflate group was easily substituted by secondary cyclic aliphatic amines. Thus, a number of new 8-amino-6-(2-R-thiazol-4-yl)-1,7-naphthyridines – previously inaccessible heterocyclic derivatives with promising biological activity – were obtained.

It has been reported that the halogen dance reaction can be used to synthesize polyfunctionalized 1,3-thiazoles. The transformation into target products was carried out by lithiation of 2-bromo-5-(1,3-dioxolan-2-yl)-1,3-thiazole with lithium diisopropylamide (LDA) followed by treatment with various electrophiles. The obtained compounds were then successfully applied to prepare novel 4,5-difunctional thiazole derivatives.

Xanthine oxidase is a known therapeutic target for the treatment of hyperuricemia and related diseases. Despite the availability of current drugs such as allopurinol and febuxostat, the search for new compounds to effectively inhibit this enzyme remains relevant. In our study, 75 virtual structures of 4‐(5‐aminosubstituted‐4‐cyanooxazol‐2‐yl)benzoic acids with structural similarity to febuxostat were designed for evaluation of their potency against xanthine oxidase. After molecular docking simulations, eight compounds were selected for synthesis and in vitro testing. The synthesized compounds were found to exhibit in vitro xanthine oxidase inhibitory activity in the nanomolar concentration range. The most effective inhibitors with 4‐benzylpiperidin‐1‐yl or 1,2,3,4‐tetrahydroisoquinolin‐2‐yl substituents at position 5 of the oxazole ring had IC50 values close to that of febuxostat. The kinetic data suggest a mixed‐type inhibition when the inhibitor binds preferentially to the free enzyme rather than to the enzyme‐substrate complex. Molecular docking and molecular dynamic simulations were carried out to get insight into the key interactions of the inhibitors bound to the xanthine oxidase active site.

Novel 2,4-disulfonylsubstituted 5-aminothiazoles were synthesized and their anticancer activity was assessed at a high dose (10 μM) against NCI 60 cancer cell lines. Compounds 24 and 25 showed the antiproliferative activity with mean growth inhibition about 66.0%. Replacing 4-hydroxypiperidine 24 with the more hydrophilic N-methyl piperazine 25 increased the number of sensitive cell lines while replacing these hydrophilic groups with lipophilic ones abolished the anticancer activity. The COMPARE analysis showed that the tested compounds had a moderate positive correlation with alkylating agents (CCNU and methyl CCNU) and with a purine nucleotide biosynthesis inhibitor analog (L-cysteine). The results indicate that the above mechanisms of antitumor action of standard compounds are not the main ones for the tested compounds due to the lack of a high correlation. The results of this study allow us to consider compounds 24 and 25 as a basis for their further functionalization to obtain more active compounds.

In this work, we synthesized a series of new 1,3-oxazole derivatives comprising the sulfonylamide group and tested their activity against the human tumor cell line panel. This study further explores the stereoelectronic characteristics of 1,3-oxazol-5-sulfonylamides and new 1-(1,3-oxazol-5-yl)piperidine-4-sulfonylamides to connect their anticancer activity to the molecular structure. Combining in vitro and in silico methods, we analyzed how the proximity of the sulfonylamide group to the heterocyclic ring affects the structure-activity interplay. Herein, our assessment is based on the purported complexation of 1,3-oxazoles with targeted biomolecular fragments involving the pi-stacking interaction and hydrogen bonding within the prospective complexes. Defining the probability of the prospective drug-target interactions, we detail conformational properties, donor/acceptor capabilities, electronic characteristics, and thermodynamic preference of produced sulfanylamide group containing 1,3-oxazoles toward biomolecular fragments, identifying the nature of variations in anticancer activity.

This research focuses on the synthesis and in vitro anticancer evaluation of functionalized 2-aryl-5-(4-piperazin-1-yl)oxazoles and 5-[(4-arylsulfonyl) piperazin-1-yl]-2-phenyloxazoles. Oxazoles are a versatile class of compounds with diverse biological activities, making them attractive targets in medicinal chemistry. We incorporated amino and sulfonamide functionalities into the oxazole scaffold, as they have shown potential for interacting with biological targets. The synthesis of target oxazole derivatives was accomplished using 2-aroylamino-3,3-dichloroacrylonitriles as starting materials and employing efficient reaction conditions. The resulting compounds exhibited structural features that make them promising candidates for further chemical modifications and biological evaluations. Additionally, a series of sulfonamides were synthesized from 5-(piperazin-1-yl)oxazole-4-carbonitrile hydrochloride, offering diverse bioactivity and versatile structural characteristics. However, no potent inhibitors of malignant cell growth were identified among the tested compounds. Nevertheless, we categorized the investigated substances into two distinct groups based on their activity profile. Group A, comprising sulfonamides, displayed pronounced anticancer activity against breast cancer and melanoma cell lines. On the other hand, group B, the 2-aryl-5-(4-R-piperazin-1-yl)oxazole-4-carbonitriles, exhibited a moderate effect primarily on renal cancer cell lines. These findings provide valuable insights for further structural modifications in the quest for more potent anticancer agents.

A novel series of N-(4-cyano-1,3-oxazol-5-yl)sulfonamides have been synthesized and characterized by IR, 1H NMR, 13C NMR spectroscopy, elemental analysis and chromato-mass-spectrometry. The anticancer activities of all newly synthesized compounds were evaluated via a single high-dose assay (10 mu M) against 60 cancer cell lines by the National Cancer Institute (USA) according to its screening protocol. Among them, compounds 2 and 10 exhibited the highest activity against the 60 cancer cell lines panel in the one-dose assay. Compounds 2 and 10 showed inhibitory activity within the GI50 parameter and in five dose analyses. However, their cytostatic activity was only observed against some cancer cell lines, and cytotoxic concentration was outside the maximum used, i. e., >100 mu M. The COMPARE analysis showed that the average graphs of the tested compounds have a moderate positive correlation with compounds with the L-cysteine analog and vinblastine (GI50) as well as paclitaxel (TGI), which target microtubules. Therefore, disruption of microtubule formation may be one of the mechanisms of the anticancer activity of the tested compounds, especially since among tubulin inhibitors with antitumor activity, compounds with an oxazole motif are widely represented. Therefore, N-(4-cyano-1,3-oxazol-5-yl)sulfonamides may be promising for further functionalization to obtain more active compounds.