Abstract
2-Phenyl-1H-indole-3-carbaldehyde-based barbituric acid, thiobarbituric acid, thiosemicarbazide, isoniazid, and malononitrile derivatives were synthesized under photochemical conditions. The antitumor activities of the synthesized compounds were evaluated on three different human cancer cell lines representing prostate cancer cell line DU145, Dwivedi (DWD) cancer cell lines, and breast cancer cell line MCF7. All the screened compounds possessed moderate anticancer activity, and out of all the screened compounds, 5-{1[2-(4-chloro-phenyl)2-oxo-ethyl]-2-phenyl-1H-indole-3-ylmethylene}-2-thioxo-dihydro-pyrimidine-4,6-dione (2b) and 5-{1[2-(4-methoxy-phenyl)2-oxo-ethyl]-2-phenyl-1H-indole-3-ylmethylene}-2-thioxo-dihydro-pyrimidine-4,6-dione (2d) exhibited marked antitumor activity against used cell lines. Additionally, barbituric acid derivatives were selective to inhibit cell line DWD and breast cancer cell lines.
Highlights
It is an alarming situation to know that over a million cases of cancer occur in the USA annually, and cancer related deaths are estimated to reach 12 million worldwide in the year 2015 [1]
In continuation of our studies on biologically active heterocyclics [3, 4], we have focused on anticancer activity of 2-phenyl-1H-indole-3-carbaldehyde derivatives
Recent literature survey reveals that antitumor activities of indole derivatives [9,10,11] possessed a unique photoresponsive activity [12] used in light-emitting electrochemical cells [13], solid-state lasers, fluorescent labels, etc. 2-Phenyl1H-indole-3-carbaldehyde derivatives inhibited the growth of MDA-MB-231 and MCF7 breast cancer cells by combining indole and barbituric acid, and new hybrid molecules were synthesized and evaluated for anticancer activity [14,15,16,17,18]
Summary
It is an alarming situation to know that over a million cases of cancer occur in the USA annually, and cancer related deaths are estimated to reach 12 million worldwide in the year 2015 [1]. In continuation of our studies on biologically active heterocyclics [3, 4], we have focused on anticancer activity of 2-phenyl-1H-indole-3-carbaldehyde derivatives. 2-Phenyl1H-indole-3-carbaldehyde derivatives inhibited the growth of MDA-MB-231 and MCF7 breast cancer cells by combining indole and barbituric acid, and new hybrid molecules were synthesized and evaluated for anticancer activity [14,15,16,17,18]. Fan Zhang et al synthesized and evaluated in vitro antitumor activity of 2-amino-3-cyano-6-(1H-indole-3-yl)-4phenylpyridine derivatives. These derivatives were screened for their cytotoxic activity against four human cell lines (A549, H460, HT-29, and SMMC-7721) and displayed an excellent antitumor activity against these cell lines [19]. Merbarone has shown a curative activity against L1210 leukemia and possessed an important activity against some other murine tumors [20, 21], but further
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
