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3‐Arylindanones and related compounds as antiproliferative agents against colorectal cancer
Author(s) -
Srivastava Ankita,
Ravi Kusumoori,
Fatima Kaneez,
Maheshwari Mayank,
Ashraf Raghib,
Hasanain Mohammad,
Yadav Pankaj,
Iqbal Hina,
Kumar Yogesh,
Luqman Suaib,
Chanda Debabrata,
Khan Feroz,
Shanker Karuna,
Sarkar Jayanta,
Negi Arvind Singh
Publication year - 2019
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13574
Subject(s) - apoptosis , colchicine , chemistry , cell cycle checkpoint , colorectal cancer , antimitotic agent , tubulin , docking (animal) , cell cycle , toxicity , colorectal adenocarcinoma , cell culture , pharmacology , cancer research , biochemistry , cancer , biology , microtubule , microbiology and biotechnology , medicine , genetics , nursing , organic chemistry
Abstract Diverse benzylidene indanones and their derivatives were synthesized as anticancer agents. Two of the analogues, that is 7 and 22, exhibited significant antiproliferative activity against several human cancer cell lines. Both the compounds possessed antimitotic activity and induced apoptosis in DLD 1 colorectal adenocarcinoma cells through activation of caspase pathways. In cell cycle analysis, both the compounds induced predominantly G2/M phase arrest in DLD 1 cells. Molecular docking studies revealed that compound 7 occupies colchicine binding pocket of β‐tubulin. Both the compounds were safe in acute oral toxicity in rodents. Both the compounds are further being optimized for better efficacy.