A series of new thiophene linked chalcone hybrids has been designed and synthesized. The key intermediate thiophene‐2‐carbaldehyde 13 was synthesized by coupling furan and phenyl ring via Suzuki reaction. The new scaffolds were synthesized by base catalyzed condensation reaction from key intermediate with various substituted acetophenones to build the chalcone core. The conversion in this synthesis involves the following steps (i) Selective bromination, (ii) regioselective Suzuki coupling (iii) Various aromatic substituents were introduced by classical aldol condensation. We screened all compounds of this thiophene‐chalcone derivatives (15 a‐n) in selected cancer cell lines viz. Human breast (MCF‐7, MDA‐MB‐453) prostate cancer (PC‐3), lung (A549). The screened compounds showed good anticancer activity on two of the studied cell lines with best IC50 values of thiophene‐chalcone derivative 15 e (6.3±0.9 μM) on A549 and with GI50 values of compound 15 e (1.9±0.3 μM) on A549 cells. This strategy is operationally simple and works with a diverse range of substrates and warrants future investigations for further anticancer drug development.
Alcaligenes sp. HPC 1271 demonstrated antibacterial activity against multidrug resistant bacteria, Enterobacter sp., resistant to sulfamethoxazole, ampicillin, azithromycin, and tetracycline, as well as against Serratia sp. GMX1, resistant to the same antibiotics with the addition of netilmicin. The cell-free culture supernatant was analyzed for possible antibacterials by HPLC, and the active fraction was further identified by LC-MS. Results suggest the production of tunicamycin, a nucleoside antibiotic. The draft genome of this bacterial isolate was analyzed, and the 4.2 Mb sequence data revealed six secondary metabolite-producing clusters, identified using antiSMASH platform as ectoine, butyrolactone, phosphonate, terpene, polyketides, and nonribosomal peptide synthase (NRPS). Additionally, the draft genome demonstrated homology to the tunicamycin-producing gene cluster and also defined 30 ORFs linked to protein secretion that could also play a role in the antibacterial activity observed. Gene expression analysis demonstrated that both NRPS and dTDP-glucose 4,6-dehydratase gene clusters are functional and could be involved in antibacterial biosynthesis.
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