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Fused pyridine derivativesFused pyridine derivatives R 0450 Synthesis of Indoloquinolones, Triazoloindoloquinolines and Its Derivatives. -A variety of novel indoloquinolones, triazoloindoloquinolines (IX) and azetidinylamino-substituted indoloquinolines [cf. (XIII)] are synthesized from hydrazinoquinolines (I) involving thermal Fischer indolization as the key step [→(V)]. Selected compounds are evaluated for their antibacterial activity. -(MULWAD*, V. V.; LOHAR, M. V.; Indian J.

Hypoxia-inducible factor-1α (HIF-1α) and signal transducer and activator of transcription 3 (STAT3) are transcription factors and are activated in response to hypoxia. Both HIF-1α and STAT3 regulate various aspects of cancer biology such as cell survival, proliferation, angiogenesis etc. and are constitutively expressed in a wide range of human cancers. In the last decade, over expression of HIF-1α and STAT3 has been demonstrated in many common human cancers, thereby emerging as highly compelling anticancer targets for drug discovery. We herein report the design and synthesis of new imidazopyridine based potent dual inhibitors of HIF-1α and STAT3 pathways. The lead compound of this series P3971 has been identified as a potent inhibitor of HIF-1α (200 nM) and STAT3 (350 nM) with significant antiproliferative activity against various cancer cell lines. Moreover, P3971 was also found to be orally efficacious in HCT116 (colon cancer) and H460 (lung cancer) xenograft mice models.

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We are herein reporting the regioselective synthesis of quinazoline containing novel monoaryl ethers (quinazoline‐O‐Ar) (3a‐3j) at room temperature without any catalyst. From commercially available 2,4‐dichloro‐6,7‐dimethoxyquinazoline (1), 4‐chloro was selectively substituted with variety of electronically rich, electronically poor and electronically neutral phenols (2a‐2j). Reaction was carried out in DMF and NaH for 4‐6 hours at room temperature in fairly good yield. The products were purified (>98% pure, hplc) by crystallization to avoid the use of column chromatography.