Bioinspired thiazolo-[2,3-b] quinazolin-6-one derivatives as potent anti-cancer agents targeting EGFR: their biological evaluations and in silico assessment.

Cancer is a challenging and second most deadly disease. The epidermal growth factor receptors (EGFRs) dimerize upon ligand bindings to the extracellular domain that intiates the downstream signaling cascades and activates intracellular kinase domain. Thus, activation of autophosphrylation through kinase domain results in metastasis, cell proliferation, and angiogenesis.

Structural insights into conformational stability and binding of thiazolo-[2,3-b] quinazolinone derivatives with EGFR-TKD and study.

Heterocyclic molecules are well-known drugs against various diseases including cancer. Many tyrosine kinase inhibitors including erlotinib, osimertinib, and sunitinib were developed and approved but caused adverse effects among treated patients. Which prevents them from being used as cancer therapeutics.

A new class of fluorogenic thiazolo[2,3-]quinazolinone receptor: selective detection towards mercury and hydrogen bisulfate ions in aqueous medium.

A series of fluorophoric and structurally diverse thiazoloquinazoline derivatives were synthesized in a one-pot multicomponent cascade reaction using a microwave irradiation technique. The unique structural arrangement of the synthesized compounds encouraged us to design a new type of bioactive molecular receptor. This receptor interacts with HSO in 1 : 1 and Hg in 1 : 2 binding stoichiometric ratios resulting in a change in fluorescence as well as absorption spectra in aqueous medium.

In Silico and In Vitro Evaluations of Fluorophoric Thiazolo-[2,3-b]quinazolinones as Anti-cancer Agents Targeting EGFR-TKD.

Epidermal growth factor receptor tyrosine kinase domain (EGFR-TKD) plays a pivotal role in cellular signaling, growth, and metabolism. The EGFR-TKD is highly expressed in cancer cells and was endorsed as a therapeutic target for cancer management to overcome metastasis, cell proliferation, and angiogenesis. The novel thiazolo-[2,3-b]quinazolinones series were strategically developed by microwave-assisted organic synthesis and multi dominos reactions aimed to identify the potent thiazolo-[2,3-b]quinazolinone inhibitor against EGFR-TKD.

Resonance assignments and secondary structure prediction of secretory protein Rv0603 from Mycobacterium tuberculosis H37Rv.

We report the NMR resonance assignments of N-terminal signal sequence deleted secretory protein Rv0603 (∆-Rv0603) from Mycobacterium tuberculosis H37Rv. ∆-Rv0603 displayed good peak yield and signal dispersion in 2D [N-H] HSQC spectrum, which prompted us to proceed for resonance assignments on this construct. Standard triple-resonance experiments for resonance assignments were recorded on [U-N]-∆Rv0603 and [U-N, C]-∆Rv0603 samples.

The construction of fluorophoric thiazolo-[2,3-]quinazolinone derivatives: a multicomponent domino synthetic approach.

Acid-mediated one-pot domino reactions of substituted 2-amino thiazoles, substituted benzaldehydes and cyclic diketones have been developed for the synthesis of novel and architecturally unique thiazolo[2,3-]quinazolinone derivatives under microwave irradiation. In this protocol, a series of thiazolo[2,3-]quinazolinone derivatives have been synthesized and the excellent fluorescence behaviors of some of the molecules have been reported based on the incorporation of different electron-donating and electron-withdrawing substituents on the aryl moieties of the target molecules.

Growth-arresting Activity of Acmella Essential Oil and its Isolated Component D-Limonene (1, 8 P-Mentha Diene) against (Microbial Type Culture Collection 296).

Background: is used as a remedy in toothache complaints by the tribal people of Western part of Odisha, India.

Objective: The objective of this study was to study the growth-arresting activity of an indigenous Acmella essential oil (EO) ( Murr, ) and its isolated component, d-limonene against (microbial type culture collection 296).

Materials And Methods: The EO was extracted from flowers of indigenous using Clevenger's apparatus and analyzed by gas chromatography-mass spectrometry (GC-MS).

Design, synthesis and cytotoxicity of novel chalcone analogs derived from 1-cyclohexylpyrrolidin-2-one and 2,3-dihydrobenzo[f]chromen-1-one.

Two divergent series of novel chalcone analogs, one derived from 1-cyclohexylpyrrolidin-2-one and the other derived from 1-benzo[f]chromanone, were designed, synthesized and evaluated for cytotoxicity against two murine cancer cell lines. Two 1-benzo[f]chromanone analogs, 4g and 4j yielded moderate toxicity against both melanoma B16 and lymphoma L1210 cell lines with IC(50) values between the range of 5 and 6 µM. With an IC(50) value of 3.

5-Benzyl-idene-3-phenyl-2-phenyl-imino-1,3-thia-zolidin-4-one.

The title compound, C(22)H(16)N(2)OS, is a chalcone analog with a thia-zolidinone core that was synthesized as a potential cytotoxic and anti-cancer agent. The structure is commensurately modulated by unit-cell doubling along the direction of the a axis of the cell. The two crystallographically independent mol-ecules are differerentiated by the dihedral angle between the mean planes of the benzyl-idene phenyl group against the thia-zolidin-4-one moiety, which is 5.