Derivatives of 3-chlorobenzo[b]thiophene-2-carboxanilides and their "cyclic" analogues benzo[b]thieno[2,3-c]quinolones were synthesized. Spectroscopic study of the interactions of some representatives of "cyclic" derivatives and their "acyclic" precursors with ds-DNA/RNA supported strong intercalative binding of the former and weak nonintercalative binding of the latter group of compounds. All tested compounds showed a certain antiproliferative effect on a series of human tumor cells and on a normal cell line. Among the compounds, those with one amidino-substituent have shown the best effect. The most active benzo[b]thieno[2,3-c]quinolones induced apparent S and G2/M arrests of the cell cycle, which resulted in apoptosis. These results strongly suggest that the compounds may act as topoisimerase "poisons", which is in good agreement with their intercalative mode of binding to ds-DNA/RNA, in contrast to the studied "acyclic"group of derivatives. 6a and 6d showed the best selectivity by inhibiting the growth of tumor cells but not of normal fibroblasts.

Purpose: Despite the well-known fact that intensity-modulation could significantly improve the dose distributions in breast irradiation, its clinical implementation has been hindered by deficiencies in the current inverse planning systems and by the lack of a comprehensive procedure. The aim of this work was to develop a general scheme of intensity-modulated breast treatment using MSRT and to demonstrate its superiority over IMRT as well as standard tangential-field (TF) technique using 20 clinical cases of various breast sizes.Methods: The patient setup and target definition were the same as that used in the TF treatment. Two planning methods were studied: (1)manual forward planning, and (2)computer MSRT optimization. A 3D planning system with a trial-and-error was used in the manual MSRT planning to stack MLC segments on top of the standard TFs to get a sensible MSRT plan. The underlying reason for the approach to be a viable choice is that the initial TFs have already brought the system to the vicinity of optimal solution. As a result, it is often sufficient to add 1∼3 segments to greatly improve the dose distribution. MSRT optimization was also developed using a gradient method. The DVH-based score function depended on both segment weights and shapes. MLC constraints were included to prevent unphysical MLC configurations. The target volume, defined at the patient setup based on the palpable breast tissue, was used by the algorithm for calculation.The segmented fields were concatenated to form a step-and-shoot delivery. An algebraic method was devised to determine the segmented MU to optimally compensate the MLC transmission. The fluence map and MU were independently checked. 20 patients were planned and the results were compared with the standard TF plans, as well as the TF and multiple-field IMRT plans.Results: The MSRT significantly improved target dose uniformity. Figure 1 shows a manual plan. It was also possible to reduce the lung/heart dose with a slight deterioration of target dose. Optimization yielded consistent beam apertures and weights and became advantageous for complicated cases. Our results revealed that MSRT could easily reduce the dose uniformity from 105∼120% (prescription was at 90%) to 100∼112%. The results were comparable or even more favorable than the conventional TF IMRT plans. It was noticed that IMRT with 3∼7 beams was inferior in that more normal tissues were irradiated.Conclusion: IMRT deviates from the conventional approach and requires additional steps in the treatment process. MSRT bridges the gap between conventional and IMRT treatments. For breast cancer, MSRT is a natural extension of standard procedure and improves the treatment without paying the excessive overhead associated with current IMRT. Purpose: Despite the well-known fact that intensity-modulation could significantly improve the dose distributions in breast irradiation, its clinical implementation has been hindered by deficiencies in the current inverse planning systems and by the lack of a comprehensive procedure. The aim of this work was to develop a general scheme of intensity-modulated breast treatment using MSRT and to demonstrate its superiority over IMRT as well as standard tangential-field (TF) technique using 20 clinical cases of various breast sizes. Methods: The patient setup and target definition were the same as that used in the TF treatment. Two planning methods were studied: (1)manual forward planning, and (2)computer MSRT optimization. A 3D planning system with a trial-and-error was used in the manual MSRT planning to stack MLC segments on top of the standard TFs to get a sensible MSRT plan. The underlying reason for the approach to be a viable choice is that the initial TFs have already brought the system to the vicinity of optimal solution. As a result, it is often sufficient to add 1∼3 segments to greatly improve the dose distribution. MSRT optimization was also developed using a gradient method. The DVH-based score function depended on both segment weights and shapes. MLC constraints were included to prevent unphysical MLC configurations. The target volume, defined at the patient setup based on the palpable breast tissue, was used by the algorithm for calculation. The segmented fields were concatenated to form a step-and-shoot delivery. An algebraic method was devised to determine the segmented MU to optimally compensate the MLC transmission. The fluence map and MU were independently checked. 20 patients were planned and the results were compared with the standard TF plans, as well as the TF and multiple-field IMRT plans. Results: The MSRT significantly improved target dose uniformity. Figure 1 shows a manual plan. It was also possible to reduce the lung/heart dose with a slight deterioration of target dose. Optimization yielded consistent beam apertures and weights and became advantageous for complicated cases. Our results revealed that MSRT could easily reduce the dose uniformity from 105∼120% (prescription was at 90%) to 100∼112%. The results were comparable or even more favorable than the conventional TF IMRT plans. It was noticed that IMRT with 3∼7 beams was inferior in that more normal tissues were irradiated. Conclusion: IMRT deviates from the conventional approach and requires additional steps in the treatment process. MSRT bridges the gap between conventional and IMRT treatments. For breast cancer, MSRT is a natural extension of standard procedure and improves the treatment without paying the excessive overhead associated with current IMRT.

The multistep synthesis of new monosubstituted amides of dibenzosuberone series is described starting from 3-bromobenzosuberone; N-(3 -dimethylaminopropyl)-10,11-dihydro-5H-dibenzo [a,d] cycloheptene-5-one-3-carboxamide 4 and N-(3 -dimethylaminopropyl)-3-chloro-dibenzosuberonyl [4',12'-b]thiophene-2-carboxamide 7.

AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

I n t r o d u c t i o n Recently, we reported the synthesis of new heteropolycyclic quinolones from corresponding anilides applying the photochemical dehydrohalogenation reaction (1). In our previous papers we reported on the usefulness of monofold photochemical dehydrocyclization reaction for preparing quinolones condensed with heterocyclic nuclei: furoquinolones (2), furo-bis-quinolones(3), benzofurophenenthr idones and benzothienophenenthridones (4). Although the photochemical dehydrohalogenation reaction improved by Castle and coworkers (5) is widely used in the preparation of condensed heterocyclic quinolones (6-10) the reaction of twofold photochemical dehydrohalogenation reaction was first introduced in our laboratory in the synthesis of heteropolycyclic diquinolones (11).

The electron impact mass spectra of some benzo[b]thiophene- and thieno[2,3-b]thiophene-2,5-dicarbonyldichlorides, 2,5-dicarbonyldianalides, 9-anilido-benzo[b]thienyl[2,3-c]quinolones and 9-anilido-thieno[4,5-b']thienyl[2,3-c]quinolones are discussed. Dominant peaks in dianilides are formed by cleavage of the C-N bond on one side of the anilide group, as well as on the anilide group itself in anilidoquinolones. These ions fragment further by the cleavage of a C-C bond in dianilides and the CONRPh group is lost directly, while the quinolonic part of the molecule in quinolones fragments with low probability. Characteristic fragment ions of dicarbonyldichlorides arise by the cleavage of the C-Cl bond,

Four new anilidoquinolones; 9-anilidobenzo [b]thieno[2,3-c] quinolin-6(5H)-one (6), 9-N'-methylanilidobenzo [b]thieno[2,3-c]-5-N-methylquinolin-6-one (7), 9-anilidothieno[4,5-b']thienyl[2,3-c]quinolin-6(5H)-one (16), and 9-N'-methylanilidothieno [4,5-b']thienyl[2,3-c]-5-N-methylquinolin-6-one (17) were prepared by photochemical dehydrohalogenation from the dianilides (4, 5, 14 and 15). Photochemical dehydrogenation of the anilides to produce multicondensed diquinolones did not occur.

Furyl- and thienylacrylates (8-14) and acrylic acids (8a, 10a-14a) are prepared in moderate yields by palladium catalysed coupling of substituted bromofurans and bromothiophenes with ethyl acrylate.

AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Electron ionization mass spectrometry is shown to provide a valid analytical tool for the structural characterization of the title compounds. Diagnostic fragmentation pathways of an unsymmetrically substituted 2,5-furan dicarbonyl dichloride and dianilide were observed.