BackgroundMen of African descent have the highest incidence and mortality rates of prostate cancer (PrCa) worldwide. Notably, PrCa is increasing in Africa with Nigerian men being mostly affected. Thus, it is important to understand risk factors for PrCa in Nigeria and build capacity for cancer research. The goals of this study were to determine the feasibility of conducting an epidemiological study of PrCa and to obtain preliminary data on risk factors for PrCa in Nigeria.MethodsA case–control study (50 cases/50 controls) was conducted at the University College Hospital (UCH) in Ibadan, Nigeria, between October 2011 and December 2012. Men aged 40 to 80 years were approached for the study and asked to provide informed consent and complete the research protocol. Logistic regression models were used to examine associations between demographic, social and lifestyle characteristics and risk of PrCa.ResultsThe participation rate among cases and controls was 98% and 93%, respectively. All participants completed a questionnaire and 99% (50 cases/49 controls) provided blood samples. Cases had a median serum diagnostic PSA of 73 ng/ml, and 38% had a Gleason score 8–10 tumor. Family history of PrCa was associated with a 4.9-fold increased risk of PrCa (95% CI 1.0 - 24.8). There were statistically significant inverse associations between PrCa and height, weight and waist circumference, but there was no association with body mass index (kg/m2). There were no associations between other socio-demographic and lifestyle characteristics and PrCa risk.ConclusionThis feasibility study demonstrated the ability to ascertain and recruit participants at UCH and collect epidemiological, clinical and biospecimen data. Our results highlighted the advanced clinical characteristics of PrCa in Nigerian men, and that family history of PrCa and some anthropometric factors were associated with PrCa risk in this population. However, larger studies are needed to better understand the epidemiological risk factors of PrCa in Nigeria.
A visible-light-induced cross-dehydrogenative methodology has been developed for the regioselective sulfenylation of pyrazolo[1,5-a]pyrimidine derivatives. Rose bengal, blue LEDs, KI, K 2 S 2 O 8 , and DMSO are all essential for this photocatalytic transformation. The protocol is applicable for the synthesis of a library of 3-(aryl/heteroaryl thio)pyrazolo[1,5-a]pyrimidine derivatives with broad functionalities. The selectivity and scalability of the methodology have been also demonstrated. Moreover, the efficiency of this strategy for sulfenylation of pyrazoles, indole, imidazoheterocycles, and 4-hydroxy coumarin has been proven. The mechanistic investigation revealed the radical-based mechanism and formation of diaryl disulfide as a key intermediate for this cross-dehydrogenative coupling reaction.
Synthesis of pharmaceutically active heterocycles is always appealing as the majority of the widely used drugs contain heterocyclic moieties as their core structure. So, the straightforward construction of heterocycles from readily available/accessible reagents is one of the prime targets of the synthetic chemists. In this context, CÀ H functionalization has emerged as an effective tool for the designing and synthesis of various heterocyclic moieties as it offers a straightforward and step-economic pathway. On the other hand, the readily available/accessible conjugated carbonyls are well-known reagents for the construction of carbocycles and heterocycles over the years. However, the employment of CÀ H functionalization of the two CÀ H bonds of the conjugated alkene in carbocycle/heterocycle synthesis was not so explored. In the last decade, much focus has been paid on the synthesis of various pharmaceutically active heterocycles through CÀ H bond functionalization of α,β-unsaturated aldehydes/ketones. These protocols have been developed through either oxida-tive coupling of conjugated carbonyls with suitable coupling partners or intramolecular CÀ H bond functionalization of conjugated carbonyls. In this review, we will discuss all the methodologies developed for the synthesis of heterocycles employing intermolecular CÀ H bond functionalization of conjugated carbonyls. The mechanistic pathways and usefulness of the methodologies will be also highlighted.
A simple and efficient visible-light-induced methodology has been developed for the selective synthesis of dihydro-4H-furo[3,2-c]chromen-4-one derivatives via dehydrogenative coupling reaction. The methodology is highly useful for the synthesis of varieties of dihydro-4H-furo[3,2-c]chromen-4-ones from readily accessible reactants under oxygen atmosphere. Importantly, the additive-free approach has been also demonstrated for this transformation. The results of the mechanistic investigation showed that this dehydrogenative reaction proceeded through a radical pathway. Additionally, the synthesized dihydro-4H-furo[3,2-c]chromen-4-one has been transformed into different 4H-furo[3,2-c]chromen-4-ones through simple protocols.
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