Design, synthesis and cytotoxicity of novel chalcone analogs derived from 1-cyclohexylpyrrolidin-2-one and 2,3-dihydrobenzo[f]chromen-1-one |
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Authors: | Brien Kimberly A Bandi Ravi Kumar Behera Ajaya Kumar Mishra Bijay Kumar Majumdar Poulomi Satam Vijay Savagian Mia Tzou Samuel Lee Megan Zeller Matthias Robles Andrew J Mooberry Susan Pati Hari Lee Moses |
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Affiliation: | Division of Natural Sciences and Department of Chemistry, Hope College, Holland, MI, USA. |
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Abstract: | Two divergent series of novel chalcone analogs, one derived from 1‐cyclohexylpyrrolidin‐2‐one and the other derived from 1‐benzo[f]chromanone, were designed, synthesized and evaluated for cytotoxicity against two murine cancer cell lines. Two 1‐benzo[f]chromanone analogs, 4g and 4j yielded moderate toxicity against both melanoma B16 and lymphoma L1210 cell lines with IC50 values between the range of 5 and 6 µM. With an IC50 value of 3.4 µM, compound 4g was also active against human MDA‐MB‐435 melanoma cells. X‐ray structures of the β‐hydroxy ketone product ( 4a ) and the α,β‐unsaturated ketone ( 4h ) were collected, and confirm the syn‐configuration between the carbonyl moiety and the β‐vinylic proton in 4h . X‐ray structures of two 1‐cyclohexylpyrrolidin‐2‐one derivatives were also obtained, and both showed an E‐configuration for the double bond. |
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Keywords: | Benzochromanone Chalcones Cytotoxicity Tubulin X‐ray |
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