Spirooxindole derivative SOID-8 induces apoptosis associated with inhibition of JAK2/STAT3 signaling in melanoma cells. [PDF]
Melanoma is generally refractory to current chemotherapy, thus new treatment strategies are needed. In this study, we synthesized a series of spirooxindole derivatives (SOID-1 to SOID-12) and evaluated their antitumor effects on melanoma.
Yan Tian+10 more
doaj +3 more sources
Benzodioxole grafted spirooxindole pyrrolidinyl derivatives: synthesis, characterization, molecular docking and anti-diabetic activity. [PDF]
A highly stereoselective, three-component method has been developed to synthesize pyrrolidine and pyrrolizidine containing spirooxindole derivatives. The interaction between the dipolarophile α,β-unsaturated carbonyl compounds and the dipole azomethine ...
Nivetha N+5 more
europepmc +2 more sources
Cancer represents a global challenge, and the pursuit of developing new cancer treatments that are potent, safe, less prone to drug resistance, and associated with fewer side effects poses a significant challenge in cancer research and drug discovery ...
Mohamed S. Nafie+9 more
doaj +2 more sources
Design, Synthesis and In Vitro Evaluation of Spirooxindole-Based Phenylsulfonyl Moiety as a Candidate Anti-SAR-CoV-2 and MERS-CoV-2 with the Implementation of Combination Studies. [PDF]
The search for an effective anti-viral to inhibit COVID-19 is a challenge for the specialized scientific research community. This work investigated the anti-coronavirus activity for spirooxindole-based phenylsulfone cycloadducts in a single and ...
Barakat A+9 more
europepmc +2 more sources
From data to discovery: leveraging big data in plant natural products biosynthesis research. [PDF]
SUMMARY Plant natural products or specialized metabolites play a vital role in drug discovery and development, with many clinically important derivatives such as the anticancer drugs topotecan (derived from the natural alkaloid camptothecin) and etoposide (derived from the natural polyphenol podophyllotoxin).
McConnachie M+4 more
europepmc +2 more sources
Simultaneous inhibition of more than one target is considered to be a novel strategy in cancer therapy. Owing to the importance of histone deacetylases (HDACs) and p53-murine double minute 2 (MDM2) interaction in tumor development and their synergistic ...
Qian Zhao+9 more
doaj +2 more sources
Two compounds, A16 and A17, were active against multidrug‐resistant Mycobacterium tuberculosis isolates (PT‐12 and PT‐20), overcoming key resistance mutations in katG and rpoB, while cytotoxicity assays confirmed that they are non‐toxic. A17 exhibited the highest antituberculosis activity, with molecular docking suggesting enoyl‐[acyl‐carrier‐protein ...
Felipe Gregório Lima+11 more
openalex +2 more sources
The tumor resistance to p53 activators posed a clinical challenge. Combination studies disclosed that concomitant administration of Bcl2 inhibitors can sensitize the tumor cells and induce apoptosis.
Yasmine M. Abdel Aziz+11 more
doaj +2 more sources
Diastereoselective Three-Component 1,3-Dipolar Cycloaddition to Access Functionalized β-Tetrahydrocarboline- and Tetrahydroisoquinoline-Fused Spirooxindoles [PDF]
A chemselective catalyst-free three-component 1,3-dipolar cycloaddition has been described. The unique polycyclic THPI and THIQs were creatively employed as dipolarophiles, which led to the formation of functionalized β-tetrahydrocarboline- and ...
Yongchao Wang+8 more
doaj +2 more sources
New spirooxindole pyrrolidine/pyrrolizidine analogs: design, synthesis, and evaluation as an anticancer agent. [PDF]
Nivetha N+5 more
europepmc +2 more sources