Pd-Catalyzed Coupling of Bromo-N-(ß-glucopyranpsyl)quinolin-2-ones with Amides: Synthesis of N-glucosyl-6BrCaQ Conjugates with Potent Anticancer Activity.

A series of N-glycosyl- 6BrCaQ conjugates was synthesized through a Pd-catalyzed cross-coupling reaction between brominated N-glycosyl quinolin-2-one derivatives and various nitrogen nucleophiles. Antiproliferative assays revealed that this new series of analogues represents a promising class of antitumor compounds as illustrated by the high biological activity observed for several derivatives towards different cancer cell lines compared to the non-glycosylated congeners.

Illuminating the breast cancer survival rates among Southeast Asian women: A systematic review and meta-analysis spanning four decades.

In Southeast Asia, breast cancer is the most prevalent cancer among women and ranks as the second leading cause of cancer-related deaths. This systematic review and meta-analysis, encompassing 27 observational cohort studies with a minimum one-year follow-up period, aimed to examine temporal trends in breast cancer survival rates. Among the subset of five out of eleven Southeast Asian nations with available data, our analysis revealed pooled survival rates of 88.8 % at 1 year, 73.8 % at 3 years, 70.8 % at 5 years, and 49.3 % at 10 years for breast cancer patients. The mean age at diagnosis was 50.77±10.07 years, with 52.81 % of patients presenting with positive lymph nodes. Notably, stages I and II remained predominant even five years post-diagnosis. Although an overall amelioration in survival rates transpired over the preceding four decades, a noticeable exception pertained to the 3-year rate, demonstrating limited improvement. These findings underscore the pressing need for enhanced research efforts, particularly in countries within the region that lack survival data, to enable accurate estimations. Furthermore, our review also emphasizes the crucial need for future comprehensive, well-designed studies to delve into the factors behind survival rate disparities in Southeast Asia and the younger age at diagnosis compared to other regions.

Synthesis and antiproliferative activity of 6BrCaQ-TPP conjugates for targeting the mitochondrial heat shock protein TRAP1.

A series of 6BrCaQ-Cn-TPP conjugates 3a-f and 5 was designed and synthesized as a novel class of TRAP1 inhibitors. Compound 3a displayed an excellent anti-proliferative activity with mean GI50 values at a nanomolar level in a diverse set of human cancer cells (GI50 = 0.008-0.30 µM) including MDA-MB231, HT-29, HCT-116, K562, and PC-3 cancer cell lines. Moreover, the best lead compound 6BrCaQ-C10-TPP induces a significant mitochondrial membrane disturbance combined to a regulation of HSP and partner protein levels as a first evidence that his mechanism of action involves the TRAP-1 mitochondrial Hsp90 machinery.

Intramolecular Pd-Catalyzed Arylation of 1-Amidosugars: A New Route to N-Glycosyl Quinolin-2-ones.

The synthesis of N-glycosylated quinolin-2-ones via an intramolecular N-arylation of glycosylamides is reported. The coupling involves the use of only Pd(OAc)2 as the catalyst and nBu4NOAc as the base in 1,4-dioxane. This versatile approach allows the synthesis of various N-glycosylated quinolin-2-ones with exclusive α or ß selectivity.

Synthesis of fused 1-aminoindole polycycles by a sequence of palladium-catalyzed N­H and C(sp2)­H arylations.

An efficient Pd-catalyzed selective intramolecular arylation of functionalized N,N'-substituted 1-aminoindoles has been reported. In all cases, the reactions take place rapidly in DMA and efficiently proceed in the presence of a Pd(OAc)2/Dpephos catalytic system, furnishing the fused indolo[2,1-a]phthalazines in high yields. Additionally, the one-pot double C­H arylation at positions C-2 and C-3 of N,N'-substituted 1-aminoindoles is effective and leads to unknown complex scaffolds of biological interest.