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951.
Application of Privileged Molecular Framework of 7‐Fluoro‐1,4‐benzodiazepin‐2‐one‐5‐methylcarboxylate to the Synthesis of Its 1‐ and 5‐Disubstituted Analogs of Medicinal Interest
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Synthetic potential of the privileged molecular framework of 7‐fluoro‐1,4‐benzodiazepin‐2‐one containing a methyl carboxylate substituent at its 5‐position was exploited to develop efficient protocols to the synthesis of several novel 5‐(1′,3′,4′)oxadiazole ring incorporated analogs of medicinal interest, appended with the Mannich's base motifs at the nitrogen atom in its seven‐membered ring. 相似文献
952.
4‐Oxo‐4H‐1‐benzopyran‐3‐carboxaldehyde (chromone‐3‐carboxaldehyde or 3‐formylchromone) 1 is an important biologically active compound. It can serve as a precursor in the synthesis of a wide range of heterocyclic systems having chromone moiety, many of which exhibit broad spectrum of biological activities such as anti‐mutagenisity, cytotoxicity, thymidine phosphorylase inhibitor, and anti‐HIV activity. During the last decade, the title compound was studied extensively. The review presents an overall survey of the synthesis, chemical reactivity, and biological activities of 4‐oxo‐4H‐1‐benzopyran‐3‐carboxaldehydes and some of its derivatives. 相似文献
953.
Sanjay Anand Kishore R. Rollakanti Ronald L. Horst Tayyaba Hasan Edward V. Maytin 《Photochemistry and photobiology》2014,90(5):1126-1135
Photodynamic therapy (PDT), in which 5‐ALA (a precursor for protoporphyrin IX, PpIX) is administered prior to exposure to light, is a nonscarring treatment for skin cancers. However, for deep tumors, ALA‐PDT is not always effective due to inadequate production of PpIX. We previously developed and reported a combination approach in which the active form of vitamin D3 (calcitriol) is given systemically prior to PDT to improve PpIX accumulation and to enhance PDT‐induced tumor cell death; calcitriol, however, poses a risk of hypercalcemia. Here, we tested a possible strategy to circumvent the problem of hypercalcemia by substituting natural dietary vitamin D3 (cholecalciferol; D3) for calcitriol. Oral D3 supplementation (10 days of a 10‐fold elevated D3 diet) enhanced PpIX levels 3‐ to 4‐fold, and PDT‐mediated cell death 20‐fold, in subcutaneous A431 tumors. PpIX levels and cell viability in normal tissues were not affected. Hydroxylated metabolic forms of D3 were only modestly elevated in serum, indicating minimal hypercalcemic risk. These results show that brief oral administration of cholecalciferol can serve as a safe neoadjuvant to ALA‐PDT. We suggest a clinical study, using oral vitamin D3 prior to PDT, should be considered to evaluate this promising new approach to treating human skin cancer. 相似文献
954.
Solid-phase organic synthesis is a rapidly expanding area of synthetic chemistry which is being widely exploited in the search for new medicinally important compounds using combinatorial techniques. In recent decades, a large number of reports related to solid-phase synthesis of heterocycles have appeared because of the wide variety in their biological activity. In this review, we report the important role of solid-phase synthesis in the synthesis of oxygen-bearing heterocycles. 相似文献
955.
Sridhar Madabhushi Kishore Kumar Reddy Mallu Raveendra Jillella Srinivas Kurva Rajpal Singh 《Tetrahedron letters》2014
A simple and efficient method for the preparation of 2,4-disubstituted quinazoline 3-oxides by reaction of a hydroxamic acid with 2-aminoaryl ketones using zinc(II) triflate as the catalyst is described. 相似文献
956.
Karthik Bharath Vladimir Pozdnyakov Dipak K. Dey 《Annals of the Institute of Statistical Mathematics》2014,66(2):369-382
We consider a combination of heavily trimmed sums and sample quantiles which arises when examining properties of clustering criteria and prove limit theorems. The object of interest, which we call the Empirical Cross-over Function, is an L-statistic whose weights do not comply with the requisite regularity conditions for usage of existing limit results. The law of large numbers, CLT and a functional CLT are proven. 相似文献
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959.
The general class of complex elliptical shape distributions on a complex sphere provides a natural framework for modeling shapes in two dimensions. Such class includes many distributions, e.g., complex Normal, Watson, Bingham, angular central Gaussian and several others. We employ this class of distributions to develop methods for asserting differences in populations of shapes in two dimensions. Maximum likelihood and Bayesian methods for estimation of modal difference are developed along with hypothesis testing and credible regions for average shape difference. The methodology is applied in an example from biometry, where we are interested in detecting shape differences between male and female gorilla skulls. 相似文献
960.