TRIAZOLOPHTHALAZINE INCORPORATING PIPERAZINE DERIVATIVES: SYNTHESIS AND IN VITRO ANTICANCER EVALUATION STUDY | ||
| Al-Azhar Journal of Pharmaceutical Sciences | ||
| Article 8, Volume 61, Issue 1, March 2020, Pages 104-116 PDF (549.62 K) | ||
| Document Type: Review Article | ||
| DOI: 10.21608/ajps.2020.86020 | ||
| Author | ||
| Hamada Abulkhair* | ||
| Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt | ||
| Abstract | ||
| Cancer remains as one of the top leading causes of death worldwide in the last decade. In an attempt to develop a potent anticancer agent, herein we are reporting the synthesis of two novel series of piperazinyltriazolophthalazines as potential anticancer agents with potential inhibitory activity against PARP-1. All the newly synthesized compounds were evaluated for their anti-proliferative activity against four human cancer cell lines namely; Hepatocellular carcinoma (HePG-2), Mammary gland breast cancer (MCF-7), Human prostate cancer (PC3) and Colorectal carcinoma (HCT-116)). The results of cytotoxicity evaluation showed that most of the synthesized compounds displayed moderate cytotoxic activity against the selected cell lines. Compound 23 showed the highest inhibitory effect followed by compound 24 against hepatocellular carcinoma (HePG2) with IC50 values of 15.05 and 17.23 µM respectively. The same two compounds also showed moderate activity against colorectal carcinoma cell line (HCT-116) with IC50 values of 21.93 and 24.06 µM respectively. | ||
| Keywords | ||
| anticancer; piperazinyltriazolophthalazines; Hepatocellular carcinoma; Mammary gland breast cancer; Human prostate cancer and Colorectal carcinoma | ||
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