99 research outputs found
5‐Substituted 1H‐Tetrazoles as Carboxylic Acid Isosteres: Medicinal Chemistry and Synthetic Methods
No full textdatacarpentry/wrangling-genomics: Data Carpentry: Genomics data wrangling and processing, June 2019
No full text<p>Data Carpentry lesson to learn how to use command-line tools to perform quality control, align reads to a reference genome, and identify and visualize between-sample variation.</p>
The Good of the Few: Reciprocity in the Provision of a Public Bad
No full textPeople have been shown to engage in favor-trading when it is efficiency-enhancing to do so. Will they also trade favors when it reduces efficiency, as in a series of wasteful public projects that each benefits an individual? We introduce the “Stakeholder Public Bad” game to study this question. In each round, contributions to a common fund increase the earnings of one person (the “Stakeholder”) but reduce the earnings of the rest of the group so much that overall efficiency is reduced. The Stakeholder position rotates through members of the group and the promise of the high reward associated with this position may enable subjects to behave reciprocally. We hypothesize that some people will help a current Stakeholder by contributing in hopes of being rewarded later with a reciprocal gift. In a lab experiment, we find evidence of such favor trading. We also find that Stakeholders in this situation seem perfectly willing to sacrifice the good of the group to reap their own personal rewards, and this is true even when their contribution decisions are public. While the revelation of information about others’ actions and roles has previously been shown to enable efficiency-increasing reciprocity, we show that it also enables efficiency-decreasing reciprocal acts. Subjects who are more risk-averse behave in a way that is more myopically self-interested as compared to less risk-averse people when information conditions preclude favor trading, and subjects who identify with the Democratic Party show more restraint when they are Stakeholder than those who do not.logrolling, social preferences, reciprocity, externalities, public bad, public good
Convenient Palladium‐Catalyzed Preparation of Primary Anilines Using a Fluorous Benzophenone Imine Reagent.
No full textConcise Enantiospecific, Stereoselective Syntheses of (+)-Crispine A and Its (−)-Antipode
No full textAn enantiospecific and stereoselective total synthesis of the natural product (+)-crispine A has been demonstrated employing a Pictet−Spengler bis-cyclization reaction between commercially available (R)-(−)-methyl 2-amino-3-(3,4-dimethoxyphenyl)propanoate and 4-chloro-1,1-dimethoxybutane to preferentially provide the cis tricyclic adduct. Decarboxylation by a convenient two-step protocol provided the enantiopure natural product in three steps with an overall isolated yield of 32% from the amino acid. The unnatural antipode (−)-crispine A was similarly prepared in three steps from the commercially available (S)-(+)-amino acid
Design, synthesis and evaluation of new indolylpyrimidylpiperazines for gastrointestinal cancer therapy
No full textHuman A3 adenosine receptor hA3AR has been implicated in gastrointestinal cancer, where its cellular expression has been found increased, thus suggesting its potential as a molecular target for novel anticancer compounds. Observation made in our previous work indicated the importance of the carbonyl group of amide in the indolylpyrimidylpiperazine (IPP) for its human A2A adenosine receptor (hA2AAR) subtype binding selectivity over the other AR subtypes. Taking this observation into account, we structurally modified an indolylpyrimidylpiperazine (IPP) scaffold, 1 (a non-selective adenosine receptors’ ligand) into a modified IPP (mIPP) scaffold by switching the position of the carbonyl group, resulting in the formation of both ketone and tertiary amine groups in the new scaffold. Results showed that such modification diminished the A2A activity and instead conferred hA3AR agonistic activity. Among the new mIPP derivatives (3–6), compound 4 showed potential as a hA3AR partial agonist, with an Emax of 30% and EC50 of 2.89 ± 0.55 μM. In the cytotoxicity assays, compound 4 also exhibited higher cytotoxicity against both colorectal and liver cancer cells as compared to normal cells. Overall, this new series of compounds provide a promising starting point for further development of potent and selective hA3AR partial agonists for the treatment of gastrointestinal cancers
ChemInform Abstract: An Efficient Synthesis of 2-Hydroxyethyl N,N,N′,N′-Tetrakis(2-chloroethyl)phosphorodiamidate.
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