5012
Mashalla Mohamed Saad El-Baroudy
synthesis of new series of furoekromone derivatives with expected antitamor sctivity
CYCLA NE/YL,so cyawde / azo / fmiedel crafts leadion / breast and liver canca cell line
For the aim of monitoring the inhibition of the growth of human cancer cells, a series of newly synthesized indole derivatives of possessing a broader spectrum of antitumor activity and fewer toxic side effects than traditional anticancer drugs have been studied. Sixteen selected indole derivatives (compounds 5b, 5c,6b,6d,7a, LL, L2,!4,!5, L}a,!flb,22a,22b,22c,22eand 23a ) were subjected to a screening systemfor investigation of their antitumor potency against breast (MCF7) and liver (HEPG2) ceil rines. Moreover, the biochemicar effects of the selected indole derivatives on some enzymes such as aspartate and alanine aminotransferase (AST and ALT) and alkaline phosphatase (ALP), in addition to albumin, globulins, creatinine, total lipids, cholesterol, triglycerides and bilirubin in serum of mice were studied in comparison to 5-Flurouracil and Doxorubicin. The antitumor activity results indicated that that the selected indole derivatives showed growth inhibition activity against the tested cell line but with varying intensities extents in comparison to the known anticancer drugs: 5-Fluorouracil and Doxorubicin. compound 16b was the most potent one against MCFT Breast carcinoma cell, while compounds 15a, 15b, 11, 22b,22c and 22e shows moderated effect against the same celt line. On the other hand, compoun d 22b show moderate effect against HEPG2 liver carcinoma cell. Moreover, results of thebiochemical investigations showed that 5-Fluorouracil and Doxorubicin caused significant changes in the level of all parameters tested while treatment with the selected compounds e&lowedslight, moderate or no significant changes' ln this study, we have identified indole derivatives as a novel multi-component reaction of indoles and formyl furochromone for the synthesis of indole derivatives as a new class of compounds related to anti-proliferative activity. The lead compound23a was the most potent in the biological assay employed (e.9.: improved growth inhibition potentia! as compared to the reference anticancer drugs). These experimental findings may provide support for the use of these novel compounds as new weapons in the fight against different types of cancer
2015
Ph.d
Minufyea
Science