Ovarian cancer is the eighth most common cancer and the fifth leading cause of cancer death among women in America. Despite low incidence, it is one of the most lethal gynecological cancers mainly due to delay in diagnosis and recurrence of cancer with chemo-resistant profile. This recurrent ovarian cancer remains a significant health problem in the United States and world-wide for women. The standard chemotherapy uses a mono/combination treatment of tubulin binding paclitaxel (PTX, Taxol) with DNA damaging platinum agents (carboplatin/ cisplatin). However, the main limitation to the clinical usefulness of both PTX and platinum agents is the high incidence of chemo-resistance. Therefore, there is an urgent need for the development of new and more effective chemotherapeutic agents to treat ovarian cancer. In continuation of our effort to discover new anticancer agents for ovarian cancer, we screened a focused set of chromenes in selected ovarian cancer cell lines (A2780, SKOV-3, OVCAR-3, TOV112D, and acquired cisplatin resistant lines, A2780-cisR, TOV112D-cisR). In vitro cell viability was assessed by the fluorescence based Alamar Blue assay. The inhibitory concentrations 50% (IC50) were determined using Origin6.0 software by employing non-linear regression analysis. Our preliminary studies identified SP-6-27 (IC50 range: 0.102± 0.006 - 2.24±0.056 µM) and SP-6-37 (IC50 range: 0.258± 0.159 - 3.61±0.049 µM) as the most potent chromene analogs. Both compounds also exhibited a potent anticancer activity towards cisplatin resistant cell lines. The findings indicate that the novel chromenes could be developed as potential therapeutic agents for ovarian cancer.

Identification of chromene based anticancer agents for ovarian cancer

251st National Meeting (2016)

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