Supplementary Figures 1-4, Methods from Halogenated Benzimidazole Carboxamides Target Integrin α₄β₁ on T-Cell and B-Cell Lymphomas

The COVID-19 pandemic precipitated a transition from face-to-face instruction to virtual teaching modalities. This transition brought about an increase in the incidence of academic dishonesty as well as the evolution of novel methods of cheating. Additionally, the use of online “help” sites as platforms that enabled academic dishonesty became more prevalent. This chapter presents a historical perspective of academic dishonesty while addressing the motivation and cultural norms that lead students to cheat. Furthermore, this chapter discusses the evolution of cheating and the role ethics plays in maintaining academic integrity.

The sudden transition from in-person to virtual learning during the spring 2020 semester posed challenges for students and faculty alike. This paper explores the techniques used by faculty to transform the chemistry and biochemistry curriculum at a Hispanic-serving institution with a significant proportion of first-generation students and the response of students to these changes. Faculty utilized an assortment of techniques, including synchronous lectures by video conference, asynchronous prerecorded lectures, online examinations with varying timing policies, and virtual office hours. A survey was completed by 332 students across 26 different courses taught by 11 faculty regarding their preferences for course delivery format and the academic and nonacademic challenges they faced. A paired samples t-test indicated a statistically significant difference in satisfaction with face-to-face instruction (M = 4.13, SD = 0.765) and satisfaction with virtual instruction (M = 3.57, SD = 0.961), t(440) = 13.30, p < 0.001, Cohen’s d of 0.63, and Cronbach’s α of 0.767. The results indicated a preference for face-to-face instruction. Open-ended survey questions identify that the primary academic challenges faced by students involved technology, understanding material, and difficulty obtaining help, while the primary nonacademic challenges were work issues, focus/motivation, and family issues. These results may inform future practices for virtual instruction.

(19)F-modified bithiazole correctors and phenylglycine potentiators of the ΔF508-CFTR chloride channel were synthesized and their function assayed in cells expressing human ΔF508-CFTR and a halide-sensitive fluorescent protein. Fluorine was incorporated into each scaffold using prosthetic groups for future biodistribution imaging studies using positron emission tomography (PET). The ΔF508-CFTR corrector and potentiator potencies of the fluorinated analogs were comparable to or better than those of the original compounds.

A course entitled "Careers in Chemistry" has been developed and implemented in the chemistry curriculum. This seminar-style class exposes students to a full spectrum of career options available to chemists by hosting outside speakers. The workings and logistics of this course and its positive impact on students are described. Survey results suggest that implementation of a similar course or seminar series at other institutions may be beneficial in exposing students to career options in chemistry.

AbstractThe title compounds are of biological interest.

A number of novel benzo-1,3-dioxolo-, benzothiazolo-, pyrido-, and quinolino-fused 5H-benzo[d]pyrazolo[5,1-b][1,3]-oxazines and 1H-pyrazoles were synthesized utilizing an easy and effective N,N-bond forming heterocyclization reaction. In so doing, the substrate scope of this heterocyclization reaction, which starts with o-nitroheterocyclic aldehydes, was expanded to provide several unique heterocyclic compounds for biological screening. This work further demonstrates the versatility of this simple, base-mediated, one-pot heterocyclization method in the construction of novel heterocycles.

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

Irradiation of 1,2-dimethyl-3-hydroxyquinolinone (DMQ) leads to excited state intramolecular proton transfer (ESIPT) generating a 3-oxidoquinolinium species which undergoes [3 + 2] photocycloaddition with dipolarophiles. A parallel, fluorescence quenching assay using a microplate format has been developed to evaluate fluorescence quenching of this species with a range of dipolarophiles.

The intramolecular nitrile oxide cycloaddition (INOC) reaction is applied to the synthesis of novel isoxazolooxazepinoindazole, benzoisoxazolodiazepinoindazolone, and spiro[isoxazoloazepine] piperidine heterocycles. Each of these targets incorporates a unique trinitrogen-containing triheterocyclic framework.

Abstract Integrin α4β1 is an attractive but poorly understood target for selective diagnosis and treatment of T-cell and B-cell lymphomas. This report focuses on the rapid microwave preparation, structure-activity relationships, and biological evaluation of medicinally pertinent benzimidazole heterocycles as integrin α4β1 antagonists. We documented tumor uptake of derivatives labeled with 125I in xenograft murine models of B-cell lymphoma. Molecular homology models of integrin α4β1 predicted that docked halobenzimidazole carboxamides have the halogen atom in a suitable orientation for halogen-hydrogen bonding. The high-affinity halogenated ligands identified offer attractive tools for medicinal and biological use, including fluoro and iodo derivatives with potential radiodiagnostic (18F) or radiotherapeutic (131I) applications, or chloro and bromo analogues that could provide structural insights into integrin-ligand interactions through photoaffinity, cross-linking/mass spectroscopy, and X-ray crystallographic studies. Cancer Res; 70(13); 5448–56. ©2010 AACR.