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

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.

SUBMITTER: Dayal N

PROVIDER: S-EPMC7513343 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature

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

Dayal Neetu N Wang Modi M Sintim Herman O HO

ACS omega 20200911 37

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 ...[more]

PMID: 32984700

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