Work

HSD1787, a Tetrahydro-3 H -Pyrazolo[4,3- f ]Quinoline Compound Synthesized via Povarov Reaction, Potently Inhibits Proliferation of Cancer Cell Lines at Nanomolar Concentrations

Year: 2020

Type: article

Abstract: Multicomponent reaction (MCR) is often used to rapidly assemble complex compounds for drug screening. Povarov MCR has been used to prepare a new library containing tetrahydro-3H-pyrazolo[4,3-f]quinoline core and the library tested against MDA-MB-231 (a triple-negative breast cancer, TNBC, cell line). A few of the tetrahydro-3H-pyrazolo[4,3-f]quinoline-containing compounds, bearing 3-aminoindazolyl group, potently inhibited MDA-MB-231. The most active compound, HSD1787, was evaluated against NCI60 cell lines and this compound inhibited melanoma, renal, breast, ovarian, and leukemia cancer cell lines with GI50 values as low as 0.1 μM. The tetrahydro-3H-pyrazolo[4,3-f]quinoline core is therefore a new scaffold that could be developed into potent anticancer therapeutics against difficult-to-treat cancers.

Source: ACS Omega

DOI: 10.1021/acsomega.0c03001

Authors: Neetu Dayal, Modi Wang, Herman O. Sintim

Institution: Purdue University West Lafayette

Language: English

Topic: Multicomponent Synthesis of Heterocycles

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: gold

Estimated APC paid: $750