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Substitution at R3 having a halogen or alkoxy group (74f–74i) brought about a slight rise in cellular potency Using the halide analogs (74g–h) showing highest the potency in the group. Further optimization led to the invention of 74i–j, with 74k as quite possibly the most Energetic compound while in the sequence (pIC50 = 6.seventy seven) with
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Hypoxia stimulates the expression of macrophage migration inhibitory factor in human vascular sleek muscle mass cells by means ofDetermined by a putative intercalation of 186 with DNA, the authors introduced a cyclopropyl group around the indazole ring to minimize planarity, which led to the invention of compound 187 with no mutagenicity in TA1537.
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