Wiley Online Library : Chemical Biology & Drug Design
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Phenotypic assessment of antiviral activity for spiro‐annulated oxepanes and azepenes

Diversity-oriented antiviral activity screening revealed adenovirus yield reduction by a structurally novel chemotype of spiro-annulated oxepanes and azepenes. Abstract Evolutionary potential of viruses can result in outbreaks of well-known viruses and emergence of novel ones. Pharmacological methods of intervening the reproduction of various...

Sat May 25, 2024 12:38
4‐Quinolinylhydrazone analogues kill Leishmania (Leishmania) amazonensis by inducing apoptosis and mitochondria‐dependent pathway cell death

Quinolinylhydrazone analogues were synthesized and exhibited leishmanicidal effect. The best compound (MHZ15) was highly selective against Leishmania amazonensis. MHZ15 induces apoptosis and mitochondria-dependent pathway cell death. MHZ15 was effective in the experimental model of cutaneous leishmaniasis. Abstract Despite efforts, available...

Wed May 22, 2024 12:17
Design, synthesis and neuroprotective biological evaluation of novel HDAC6 inhibitors incorporating benzothiadiazinyl systems as cap groups

Novel HDAC6 inhibitors incorporating benzothiadiazinyl systems as neuroprotective agents. Abstract Histone deacetylase 6 (HDAC6), as the key regulatory enzyme, plays an important role in the development of the nervous system. More and more studies indicate that HDAC6 has become a promising therapeutic target for CNS diseases. Herein we designed...

Wed May 22, 2024 12:17
Evaluation of a panel of furochromenones as the activator and inhibitor of tyrosinase

The study screened and identified furochromenones that impact tyrosinase activity. One of the furochromenones (3k) inhibited while another (4f) stimulated tyrosinase. Abstract Tyrosinase is a copper-containing enzyme involved in the biosynthesis of melanin pigment. While the excess production of melanin causes hyperpigmentation of human skin,...

Sat May 18, 2024 12:11
Novel carbamodithioate regulates cellular hypoxia through chemical activation of prolyl hydroxylase‐2 for breast cancer chemoprevention

BBAP-6 was identified as an inducer of PHD-2 and was found to reinstate apoptosis in MCF-7 cells in-vitro as well as in DMBA-induced mammary gland carcinoma in vivo. All in all, according to the current study's findings, BBAP-6 upregulated PHD-2 and, when combined with TPZ, exhibited greater chemopreventive potential. Abstract Inhibition of prolylhydroxylase-2...

Sat May 11, 2024 12:07
Comparison of feline and human immunodeficiency virus reverse transcriptase enzymes through chemical screening and computational analysis

Feline immunodeficiency virus (FIV), is a common infection found in domesticated and wild cats worldwide. We employ a chemo-centric approach to assess the similarity between FIV-RT and HIV1-RT using experimental screening and computational chemistry methods. Through this, we identify more potent inhibitors and gain a better appreciation of FIV-RT...

Fri May 10, 2024 12:18

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