Recently I am researching about FEATURING MORPHOLINE MOIETY; NATIONAL-CANCER-INSTITUTE; BIOLOGICAL EVALUATION; PHOSPHOINOSITIDE 3-KINASE; COLORIMETRIC ASSAY; DRUG DISCOVERY; CELL-CYCLE; PI3K-ALPHA; CYTOTOXICITY; CHEMOTHERAPY, Saw an article supported by the . Published in ACADEMIC PRESS INC ELSEVIER SCIENCE in SAN DIEGO ,Authors: Helwa, AA; El-Dydamony, NM; Radwan, RA; Abdelraouf, SM; Abdelnaby, RM. The CAS is 100-83-4. Through research, I have a further understanding and discovery of 3-Hydroxybenzaldehyde. Product Details of 100-83-4
Two series of novel morpholinopyrimidine derivatives were synthesized and screened for their in-vitro cytotoxic activity against 60 tumor cell line by the National Cancer Institute, USA. The in-vitro cytotoxic IC50 values for the most active compounds 6e, 6g, and 6l against the most sensitive cell line leukemia SR were estimated (IC50 = 0.76, 13.59, and 4.37 uM, respectively). To investigate their PI3K enzyme inhibition activity, the assay was done on Class IA (alpha, beta, & delta) isoforms. The IC50 values were very promising: compound [6e = 11.73 (alpha), 6.09 (beta), 11.18 (delta)], compound [6g = 8.43 (alpha), 15.84 (beta), 30.62 (delta)], and compound [6l = 13.98 (alpha), 7.22 (beta), 10.94 (delta)], compared to the reference compound LY294002 = 6.28 (alpha), 4.51 (beta), 4.60 (delta) uM, respectively. Moreover, cell cycle analysis and annexin V-FITC staining were done on Leukemia SR, there was arrest at G2/M phase and apoptosis was induced. Finally, docking study was performed to analyze the interactive mode of these derivatives in PI3K alpha ATP-binding site. These outcomes proved that compounds 6e, 6g, and 6l are potential leads for further optimization as antileukemic agents.
About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Helwa, AA; El-Dydamony, NM; Radwan, RA; Abdelraouf, SM; Abdelnaby, RM or concate me.. Product Details of 100-83-4
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles