In an attempt to develop potent anti-cancer agents, a new 1,3,4-substituted-thiadiazole derivatives (8b-g), starting from 4-substituted-thiazol-2-chloroacetamides (4b-g), were synthesized and evaluated for their cytotoxic effects on multiple human cancer cell lines, including the hepatocellular carcinoma (HEPG-2), human lung carcinoma (A549), human breast carcinoma (MCF-7) and pseudo-normal human embryonic liver (L02) cancer cell lines by an MTT assay. Among all synthesized compounds, compound 8d showed the potent anti-cancer activities with GI values of 2.98, 2.
View Article and Find Full Text PDFTuberculosis remains a global health threat, with increasing infection rates and mortality despite existing anti-TB drugs. The present work focuses on the research findings regarding the development and evaluation of thiadiazole-linked thiazole derivatives as potential anti-tuberculosis agents. We present the synthesis data and confirm the compound structures using spectroscopic techniques.
View Article and Find Full Text PDFHeterocycles are the main structural motif of DNA and RNA and play a crucial role in various chemical reactions of metabolisms. Therefore, heterocyclic compounds show good physiological and pharmacological properties. Coumarin and pyrazole scaffolds are present in many commercial drug molecules and natural products.
View Article and Find Full Text PDFJ Chromatogr B Analyt Technol Biomed Life Sci
December 2019
We have recently introduced a non-chromatographic alternative for antibody (Ab) purification, one which does not require the use of Protein A. With this approach, polyclonal human or mouse immunoglobulins (IgG's) are captured almost quantitatively by Tween-20 micelles conjugated with a [chelator:divalent metal cation] complex. Target IgG structure remains native even following extraction from the surfactant aggregate.
View Article and Find Full Text PDFThe dearth of high quality, three dimensional crystals of membrane proteins, suitable for X-ray diffraction analysis, constitutes a serious barrier to progress in structural biology. To address this challenge, we have developed a new crystallization medium that relies on the conjugation of surfactant micelles via base-pairing of complementary hydrophobic nucleosides. Base-pairs formed at the interface between micelles bring them into proximity with each other; and when the conjugated micelles contain a membrane protein, crystal nucleation centers can be stabilized, thereby promoting crystal growth.
View Article and Find Full Text PDFA novel, one-pot, and highly facile protocol has been devised for an easy access of a series of novel glycosyl carboxamides from aldehydes using diacetoxyiodobenzene in the presence of ionic liquid at ambient temperature.
View Article and Find Full Text PDFA facile and high-yielding protocol for diverse benzotriazoles through intramolecular N-arylation of different -chloro-1,2,3-benzotriazenes using CuI/CsCO has been developed.
View Article and Find Full Text PDFLeishmaniasis, a vector-borne parasitic disease resulting from infection of macrophages by obligate intracellular parasites of genus Leishmania, has been considered a major tropical disease by the World Health Organization. Generic pentavalent antimonials have been the mainstay for therapy in the endemic regions because of its efficacy and cost effectiveness. However, the growing incidence of resistance for the pentavalent antimony complex in endemic and non-endemic regions has seriously hampered their use in these regions.
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