1. INTRODUCTION - BIOLOGICAL BACKGROUND Vindoline (1) and catharanthine (2) belonging to Vinca alkaloids (Fig. 1) are significant and representative members of indole alkaloids. They were isolated firstly from the periwinkle Catharanthus roseus being indigenous to Madagascar. Both are the base components of dimeric vinblastine (3) and vincristine (4), which have been used as original antitumor drugs since long ago [1, 2]. Vinca alkaloids were discovered in the 1950s. Unfortunately, it turned out soon that the major alkaloid in the leaves, vindoline (1),ABSTRACT The chemistry and pharmacology of the important Vinca alkaloids such as vinblastine and vincristine used in anticancer therapy are still investigated widely. Several new derivatives, e.g., vinflunine, vinorelbine, and vindesine, have been synthesized and become successful medicines in anti-cancer therapy. In 2012, we published a paper that reviewed the Vinca derivatives. Nevertheless, the interest in the preparation of new modified structures is not decreasing either in recent years. In this review, the vinblastine-type molecules with several substituents, e.g., amide, nitrile, hydrazide, substituted side chains, etc. in different positions of catharanthine and/or vindoline cores are presented. An important part of the review is the derivatization of the monomer alkaloid vindoline, which possesses no antitumor effect. Additionally, new hybrid molecules of these alkaloids are also discussed in this mini-review.