A5038081770- Histone Deacetylase Inhibitors Research
- Peptidase Inhibition and Analysis
- Protein Degradation and Inhibitors
- Click Chemistry and Applications
- Synthesis and Biological Evaluation
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthesis and Catalytic Reactions
- Epigenetics and DNA Methylation
- Nuclear Receptors and Signaling
- Bacterial biofilms and quorum sensing
- Catalytic C–H Functionalization Methods
- Inhalation and Respiratory Drug Delivery
- Synthesis and biological activity
- Organic Chemistry Cycloaddition Reactions
- Effects and risks of endocrine disrupting chemicals
- RNA modifications and cancer
- Cancer-related Molecular Pathways
- RNA Research and Splicing
- Antifungal resistance and susceptibility
- Enzyme function and inhibition
- Chemistry and Chemical Engineering
- Cholinesterase and Neurodegenerative Diseases
- Synthesis and Characterization of Pyrroles
- Computational Drug Discovery Methods
Birla Institute of Technology and Science, Pilani
2019-2025
Birla Institute of Technology and Science - Hyderabad Campus
2019-2022
University of Hyderabad
2019-2020
Institut Teknologi dan Sains Mandala
2019
National Chemical Laboratory
2016
HDAC3 modulation shows promise for breast cancer, including triple-negative cases. Novel pyrazino-hydrazide-based inhibitors were designed and synthesized. Lead compound 4i exhibited potent inhibition (IC50 = 14 nM) with at least 121-fold selectivity. It demonstrated strong cytotoxicity against cancer cells (IC50: 0.55 μM 4T1, 0.74 MDA-MB-231) normal cell toxicity. Metabolically stable displayed a superior pharmacokinetic profile. A dose-dependent therapeutic efficacy of was observed in...
The importance of HDAC3 in transcriptional regulation genes associated with long-term memory is well established. Here, we report a novel inhibitor, PT3, an excellent blood–brain barrier permeability and ability to enhance mouse model object recognition (NOR). PT3 exhibited higher selectivity for over HDAC1, HDAC6, HDAC8 compared the reference compound CI994. has significant distribution into brain tissue Cmax at 0.5 h t1/2 2.5 h. Treatment significantly improved discrimination index C57/BL6...
Bacteria regulate their phenotype, growth and population via a signalling pathway known as quorum sensing. In this process, bacteria produce molecules (autoinducers) to recognize density. Inhibiting sensing is one of the potential methods treat bacterial infection. 2-Aminobenimdazoles are reported be strongest inhibitors against wild-type P. aeruginosa. 1,2,3-Triazole based acyl homoserine lactones found good LasR receptor. Hence, in our current study, forty 1,2,3-triazole...
The selected nicotinamide-based HDAC<italic>i</italic> displayed selectivity towards HDAC3 over pan HDAC and exhibited potent cytotoxicity against the used cell lines.
Abstract A series of novel 8‐bromo‐1 H ‐1,2,3‐triazol‐4‐yl‐2‐methylquinoline derivatives and their Suzuki coupling products were synthesized via Copper catalyzed azide‐alkyne cycloaddition (CuAAC) strategy followed by microwave assisted for the development new anticancer agents. The invitro activity compounds screened against human breast cancer (MDA‐MB‐231) melanoma cell lines (B16F10). Among these, 5 c (Azetidine), e (Nitro benzoate), f (fluorobenzyl)‐1 ‐pyrazole), g (Boc piperidine), 6 a...
Abstract A linear route for the preparation of chromeno‐thio/furo‐pyridine system as potential analogs anticancer compound lamellarin D is reported in this paper. The target molecules were obtained modest to good yields by using FeCl 3 catalyzed modified Pictet‐Spengler reaction crucial final step. Compounds bearing furan rings showed higher overall yield compared their thiophene congeners. Final subjected activity screening against three different cancer cell lines. fused better activity,...
A novel 4-(1-phenyl-1-hydroxyethyl)-1-(<italic>o</italic>-hydroxyphenyl)-1<italic>H</italic>-1,2,3-triazole was designed by integrating the structural features of triazole PITENIN anticancer agents and azole class antifungal drugs.
Aim: Literature reports suggest spirochromanone derivatives exhibit anticancer activity. Methodology: The authors designed and synthesized 18 (Csp 1–18). compounds were characterized evaluated for activity against human breast cancer (MCF-7) murine melanoma (B16F10) cell lines. Results: ranged from 4.34 to 29.31 μm. most potent compounds, Csp 12 18, less toxic the embryonic kidney (HEK-293) line ∼ two/∼fourfold selective toward MCF-7 than B16F10 in comparison reference, BG-45. caused 28.6%...
The classification of bisphenol A (BPA) as an industrial endocrine disruptor has led to a ban this ubiquitous critical starting material from food and medical applications. Thus, scientists worldwide are researching develop non-ER binding compounds fulfill unmet market needs. In line with trending research topic, the current paper highlights development tetrazole derivatives bearing structure (TbB) novel weak binder or potential inactive estrogen receptor (ER) androgen (AR). ligand-based...