Drug discovery in targeted nucleic acid therapeutics encompass several stages and rigorous challenges owing to less specificity of the DNA binders and high failure rate in different stages of clinical trials. In this perspective, we report newly synthesized ethyl 4-(pyrrolo[1,2-a]quinolin-4-yl)benzoate (PQN) with minor groove A-T base pair binding selectivity and encouraging in cell results. This pyrrolo quinolin derivative has shown excellent groove binding ability with three of our inspected genomic DNAs (cpDNA 73 % AT, ctDNA58% AT and mlDNA 28 % AT) with varying A-T and G-C content.
View Article and Find Full Text PDFApproximately 140 million years ago, the Indian plate separated from Gondwana and migrated by almost 90° latitude to its current location, forming the Himalayan-Tibetan system. Large discrepancies exist in the rate of migration of Indian plate during Phanerozoic. Here we describe a new approach to paleo-latitudinal reconstruction based on simultaneous determination of carbonate formation temperature and δ(18)O of soil carbonates, constrained by the abundances of (13)C-(18)O bonds in palaeosol carbonates.
View Article and Find Full Text PDFA new and efficient protocol to synthesize substituted benzo[b]carbazole derivatives has been demonstrated involving iron-catalyzed domino isomerization/cyclodehydration sequences from substituted 2-[(indoline-3-ylidene)(methyl)]benzaldehyde derivatives. The substrates could be easily made via Pd-catalyzed domino Heck-Suzuki coupling from 2-bromo-N-propargylanilide derivatives in high yields. Notably, the generality and efficiency of this two-stage domino strategy was further exemplified by the synthesis of a polycyclic benzofuran derivative.
View Article and Find Full Text PDFIn this study we have developed an efficient synthesis of 1,2-dihydroquinoline and dihydrobenzo[b]azepine derivatives involving the iron(III) chloride intramolecular alkyne-carbonyl metathesis reaction for the first time. Various functionalized 1,2-dihydroquinolines and dihydrobenzo[b]azepines were prepared from easily accessible substrates in the presence of environmentally friendly and inexpensive iron(III) chloride (10 mol%) under mild conditions. The method is applicable to a wide range of substrates containing different functional groups and furnishing products in good to excellent yields.
View Article and Find Full Text PDFAn efficient synthesis of dibenzo[b,f]oxepines and benzo[b]oxepines via FeCl3-catalyzed alkyne-aldehyde metathesis reaction is described. Structurally diverse dibenzo[b,f]oxepines and benzo[b]oxepines have been achieved in good yields with high regio- and chemoselectivity under mild conditions. Notably, among the various catalysts such as Fe(III), Au(III), In(III), Zn(II), Ag(I) and triflic acid, the alkyne-aldehyde metathesis reaction of 2-(2'-phenylethynyl-phenyloxy)-benzaldehyde is only catalyzed by environmentally friendly and sustainable iron(III) chloride.
View Article and Find Full Text PDFAn efficient synthesis of functionalized phenanthrenes has been developed for the first time involving an iron(III)-catalyzed intramolecular coupling of 2'-alkynyl-biphenyl-2-carbaldehydes. A broad range of functionalized phenanthrene derivatives could be obtained in the present method in moderate to good yields with high chemo- and regioselectivity. This transformation can also be applied to the synthesis of an angularly fused tetracyclic compound.
View Article and Find Full Text PDFAn iron-catalyzed intramolecular alkyne-aldehyde metathesis strategy of the alkynyl ether of salicylaldehyde derivatives has been developed which works under mild reaction conditions to produce the functionalized 2H-chromene derivatives. This protocol is compatible toward a wide range of functional groups, such as methoxy, fluoro, chloro, bromo, and phenyl groups. This method provides an atom-economical and environmentally friendly approach for the synthesis of a series of substituted 2H-chromenes.
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