Anti-cancer agents in medicinal chemistry · 2023
Novel Synthetic Indazoles Abrogate Angiogenesis in Erlich Ascites Tumor Bearing Mice.
СтатьяПоддержка исследования: вне правительства СШАНазвание и аннотация: Перевод в очереди
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Ashwini Nanjundaswamy, Balaji Kyathegowdanadoddi S, Sadashivaiah Bettadahalli L, Swaroop Toreshettahally R, Jayarama Shankar, Mantelingu Kempegowda, Rangappa Kanchugarakoppal S
Аннотация
BACKGROUND: Indazoles are known for their anti-cancer properties.
OBJECTIVE: The current investigation was on the synthesis and evaluation of novel indazole derivatives for their anticancer properties.
METHODS: A series of novel indazoles were synthesized and characterized by IR, NMR and LCMS. We performed cytotoxic studies for all synthesized compounds on different cell lines such as HeLa, MCF-7 and EAC using MTT assay. The lead compound was tested further for its anti-tumor and anti-angiogenic effect on EAT tumor model.
RESULTS: Amongst the series of compounds synthesized, compound KA8 showed potent antiproliferative effect against Hela, MCF-7 and EAC cell lines with IC50 values 10.4 to 11.5 and 13.5 μM respectively. In addition, our compound KA8 significantly decreased the cell viability, body weight, ascites volume and it also showed superior survival ability of mice compared to control groups. Furthermore, it suppressed the formation of neovasculature in the peritoneum of EAT-bearing mice.
CONCLUSION: The findings reveal that the lead compound KA8 possesses potent anti-tumor and anti-angiogenic properties thereby promising it to be developed as a novel anticancer agent with further mechanistic studies.
OBJECTIVE: The current investigation was on the synthesis and evaluation of novel indazole derivatives for their anticancer properties.
METHODS: A series of novel indazoles were synthesized and characterized by IR, NMR and LCMS. We performed cytotoxic studies for all synthesized compounds on different cell lines such as HeLa, MCF-7 and EAC using MTT assay. The lead compound was tested further for its anti-tumor and anti-angiogenic effect on EAT tumor model.
RESULTS: Amongst the series of compounds synthesized, compound KA8 showed potent antiproliferative effect against Hela, MCF-7 and EAC cell lines with IC50 values 10.4 to 11.5 and 13.5 μM respectively. In addition, our compound KA8 significantly decreased the cell viability, body weight, ascites volume and it also showed superior survival ability of mice compared to control groups. Furthermore, it suppressed the formation of neovasculature in the peritoneum of EAT-bearing mice.
CONCLUSION: The findings reveal that the lead compound KA8 possesses potent anti-tumor and anti-angiogenic properties thereby promising it to be developed as a novel anticancer agent with further mechanistic studies.