This paper discusses the landmark anthelminthic substancestraditional medicine components, different categories of pluripotential synthetic and naturally occurring compounds. Much attention is paid to the sections devoted to recent discoveries (Emodepside, Monepantel, Derquantel, Tribendimidine) and to some promising works. This review focused on some aspects of molecular mechanisms of action of anthelminthic substances and of helminth adaptation to anthelminthic substances, and on alternative worming treatment options. A new substance development, be it designing a new compound or identification of properties of any existing compounds, is a time-consuming and expensive process. Application of the diversification (different types of compounds) and the focused (related compounds) screenings, software-based evaluation of anthelminthic activity in silico, chemical and genetic trials on model small animals (nematodes Artemia salina, Caenorhabditis elegans, etc.) are intended to accelerate introduction of new substances. Further knowledge in molecular action mechanisms of anthelminthic agents and in resistance development would improve planning of helminthoses control protocols. Based on the systemic analysis of particular features of the chemical structure of anthelminthic substances, the hypothesis on the viability of the targeted search for such compounds among the derivatives of conditionally progenitor cyclic hydrocarbons benzene, indene, naphthalene, 1Н-cyclopenth [a]-naphthalene, anthracene and phenanthreneby alternating absolutely unsaturated and saturated structures, including heterocyclic analogues containing nitrogen, oxygen and sulfur and different substitutes and functional groups, was voiced.