Browsing by Author "Sawant, D.M."

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    Exploration of Pd-catalysed four-component tandem reaction for one-pot assembly of pyrazolo[1,5-c]quinazolines as potential EGFR inhibitors
    (Academic Press Inc., 2019) Ansari, A.J; Joshi, G; Yadav, U.P; Maurya, A.K; Agnihotri, V.K; Kalra, S; Kumar, R; Singh, S; Sawant, D.M.
    A series of pyrazolo[1,5-c]quinazolines as EGFR inhibitors was designed and synthesized by highly efficient and novel multicomponent route involving Pd-catalyzed tandem one-pot four-component reaction. The reaction proceeds with good functional group tolerance under a simple condition with excellent regioselectivity and high efficiency. Target compounds were screened against cancer cell lines MDA-MB-231, A549 and H1299. Of these, 9b and 10b exhibited superior anticancer activity (IC50 < 2.5 ?M) to erlotinib and gefitinib. Synthetics were able to inhibit EGFR mediated kinase activity, induced ROS in cancer cells promoting mitochondrial mediated apoptosis via halting cell cycle progression at G1 phase.
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    Pd-Catalyzed Four-Component Sequential Reaction Delivers a Modular Fluorophore Platform for Cell Imaging
    (American Chemical Society, 2019) Ansari, A.J; Joshi, G; Sharma, P; Maurya, A.K; Metre, R.K; Agnihotri, V.K; Chandaluri, C.G; Kumar, Raj; Singh, S; Sawant, D.M.
    A Pd-catalyzed cascade reaction of four versatile privileged synthons is described. The sequential reaction involves the formation of five new chemical bonds by concatenating three distinct chemical steps. One of the derivatives exhibited absorption in the visible region, fluorescence with a high quantum yield, and excellent photostability. Its application is explored in live cell imaging, which exhibited cytoplasmic and mitochondrial specific staining with no toxicity. © 2019 American Chemical Society.
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    Relay tricyclic Pd (ii)/Ag (i) catalysis: design of a four-component reaction driven by nitrene-transfer on isocyanide yields inhibitors of EGFR.
    (Royal Society of Chemistry, 2018) Sawant, D.M.; Sharma, S; Pathare, R.S; Joshi, G; Kalra, S; Sukanya, S; Maurya, A.K.; Metre, R.K; Agnihotri, V.K.; Khan, S.; Kumar, Raj; Pardasania, R. T.
    Synthesis of pyrazolo[1,5-c]quinazolines from four easily available precursors is presented through a one-pot tricyclic Pd(II)/Ag(I) relay catalysis. The bimetallic relay cascade forges five new chemical bonds by concatenating six discrete chemical steps. The relay catalysis enables four-component assembly of pyrazolo[1,5-c]quinazolines that selectively inhibit EGFR, exhibit apoptosis through the ROS-induced mitochondrial-mediated pathway, and arrest the cell cycle at the G1 phase.